inhibitors

1. Kinase Inhibitors

2. Protein Phosphatase Inhibitors

3. Inhibitor Cocktail Sets

4. Calcium Signaling related Inhibitors

5. Ion Channel-related Blockers

(1) Calcium Channel Blockers

(2) Potassium Channel Blockers

(3) Sodium Channel Blockers

(4) Transient Receptor Potential (TRP) Channel Blockers

(5) Acid-Sensing Ion Channel Blockers

(6) Nicotinic Acetylcholine Receptor Blockers

(7) Other Blockers

6.G-protein Signaling and Second Messenger-related Inhibitors

7.Neurotransmitter Inhibitors

(1) Glutamate Receptor Antagonists

(2) Inhibitors of Angiotensin Conversion Enzyme

(3) Cannabinoid Receptor Antagonists

(4) GABA Receptor Antagonists

(5) Serotonin-related Inhibitors

(6) Dopamine Receptor Antagonists

(7) Noradrenaline-related Inhibitors

(8) Alzheimer's Disease Research

Alphabetical index

print (3.8 MB)   

1. Kinase Inhibitors

Product Name

Wako Cat. No.

Pkg. Size

Grade/Manufacturer

CAS No.

Soluble in

IC50

Storage Condition

Summary

A-83-01 【TGF-β R I Kinase Inhibitor IV】

018-22521

 2 mg

for Cellbiology

909910-43-6

DMSO

-

Keep at -20°C.

014-22523

10 mg

<Protein kinase inhibitor>

Selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7. Inhibits Smad2/3
phosphorylation and TGF-β-induced epithelial-to-mesenchymal transition. This product has little or no effect on bone morphogenetic protein
type I receptors, p38 MAP kinases, and extracellular-regulated kinases.

17-AAG, 97.0+ % (HPLC)

012-20101

1 mg

for Cellbiology

75747-14-7

DMSO, methanol

EC50 of HSP90 = 7.2 μM

Keep at -20°C.

<Protein kinase inhibitor/ protein tyrosine kinase (PTK) inhibitor>

Synthetic derivative of geldanamycin, which is one of the ansamycin antibiotics. 17-AAG inhibits the function of HSP90 by binding to the ATP
binding site of HSP90. HSP90 inhibitors dephosphorylate Akt resulting in inactivation of Akt and apoptosis.

AG 490, 95+% (TLC)

013-17181

5 mg

for Biochemistry

134036-52-5

DMSO, DMF,
methanol

IC50 of Dephosphorylation of EGF
receptor tyrosine kinase: 1.2 μmol;

EGF dependent cell proliferation: 6 μmol

Keep at -20°C.

<PTK inhibitor>

Specific and potent JAK-2 protein tyrosine kinase inhibitor. Also inhibits EGF receptor autophosphorylation.

AG 1296

016-20121

5 mg

for Cellbiology

146535-11-7

DMSO

-

Keep at -20°C.

<PTK inhibitor>

It inhibits signaling in human PDGF (platelet-derived growth factor) α receptor, PDGF β receptor, stem cell stimulating factor c-kit and FGF
(fibroblast growth factor) receptor.

AG 1478

017-20151

5 mg

for Cellbiology

175178-82-2

DMSO

-

Keep at -20°C.

<PTK inhibitor>

Potent and selective inhibitor of EGF receptor kinase. Decrease in EGF-stimulating DNA synthesis and inhibition of activation of EGF-
dependent src family kinase have been reported.

ALK5 Inhibitor, 96.0+ % (HPLC)

012-23021

1 mg

for Cellbiology

446859-33-2

methanol

-

Keep at -20°C.

<Protein kinase inhibitor>

Potent and selective ATP-competitive inhibitor of TGF-β RI kinase/ALK5. Can be used as substitute of Sox2 or c-Myc (Yamanaka 4 factors)
in induction of murine iPS cells.

Aminogenistein, 90.0+ % (HPLC)

017-15901

1 mg

for Biochemistry

132018-32-7

Ethanol, DMSO

IC50 of lck = 1.2 μM

Keep at -20°C.

<PTK inhibitor>

Inhibitor of PTK, especially p56lck. The product, even among other flavons, is able to specifically inhibit lck activity at a low dose and is
therefore employed as an useful tool for clarification of the mechanism of immune response activation.

Apigenin, 95+ % (TLC)

010-18914

 5 mg

for Biochemistry

520-36-5

Methanol

-

Keep at 2-10°C.

016-18911

10 mg

012-18913

50 mg

<MAP kinase inhibitor>

Plant flavonoid. It changes phenotypes of many ras transformed cells to the original form. This is achieved by inhibition of signal transduction
route mediating MAP (Miogen Activated Protein) kinase (MAPK). In case of NIH3T3 cells transformed by v-H-ras, treatment with apigenin (12.5
μM) induces dephosphorylation of p44 MAPK resulting in a decrease in MAP kinase activity.

AS 604850, 98.0+ % (HPLC)

015-23131

5 mg

for Cellbiology

648449-76-7

DMSO

IC50 of PI3Kα: 4.5 μM; PI3Kγ: 250 nM;
PI3Kβ, PI3Kδ: 250 nM

Keep at 2 - 10°C

<Protein kinase inhibitor>

Thiazolidine-dione compound, which is a potent, cell permeable and ATP-competitive inhibitor of PI3K γ. It exhibits highly selectivity.

AS 6 t05240, 95.0+ % (HPLC)

012-23141

5 mg

for Cellbiology

648450-29-7

DMSO

IC50 of PI3Kα: 60 nM; PI3Kγ: 270 nM;
PI3Kβ: 8 nM; PI3Kδ: 300 nM

Keep at 2 - 10°C

<Protein kinase inhibitor>

Thiazolidine-dione compound, which is a potent, cell permeable and ATP-competitive inhibitor of PI3K γ (Ki = 180 nM). It exhibits highly
selectivity.

ATM Kinase Inhibitor, 97.0+ % (HPLC)

015-22911

2 mg

for Cellbiology

587871-26-9

Ethanol

ATM: IC50 = 13 nM; Ki = 2.2 nM

Keep at -20°C.

<Cyclin-Dependent Kinase (CDK) Inhibitor>

Cell-permeable, ATP-competitive inhibitor of ATM kinase. Shows high ATM kinase selectivity for PIKK and PI3K family kinases.

6-Bromoindirubin-3'-oxime 【BIO】 【GSK-3 Inhibitor IX】, 95.0+ % (HPLC)

029-16241

1 mg

for Cellbiology

667463-62-9

-

-

Keep at 2 - 10°C

<Protein kinase inhibitor>

Potent and reversible ATP-competitive inhibitor. It shows to activate the Wnt signaling pathway and maintain pluripotencies in human and
murine ES cells and also promotes cardiomyocyte proliferation and acts as a GSK-3 inhibitor.

Butein, 98.0+ % (HPLC)

027-14461

10 mg

for Biochemistry

487-52-5

Methanol, DMSO

-

Keep at -20°C.

<Protein tyrosine kinase (PTK) inhibitor>

Tyrosine kinase inhibitor isolated from plant polyphenols. Reported to activate SIrt1 (Class III HDAC).

Calphostin C, 95.0+ % (HPLC)

030-15133

 50 μg

for Cellbiology

121263-19-2

DMSO, DMF

IC50 of PKC: 50 nM; HeLa S3: 0.23 μg/mL;
MCF-7: 0.18 μg/mL

Keep at 2-10°C.

034-15131

100 μg

<Protein kinase C (PKC) inhibitor>

Specific protein kinase C (PKC) inhibitor. Shows strong anticellular activity against a variety of cultured cells.

Carbonyl Cyanide m-Chlorophenylhydrazone, 97+% (TLC)

034-16993

100 mg

for Biochemistry

99534-03-9

Ethanol, acetone

-

Keep at -20°C.

038-16991

1 g

<Protein kinase inhibitor>

Potent uncoupler of oxidative phosphorylation that inhibits mitochondrial function.

CKI-7 Dihydrochloride, 97.0+ % (HPLC)

034-21501

5 mg

for Cellbiology

-

Water

-

Keep at -20°C.

<Protein kinase inhibitor>

Casein kinase (CK1) inhibitor. Use with SB431542 and Y-27632 induces differentiation of human ES cells and human iPS cells into retinal
progenitor cells in serum- and feeder cell-free culture medium.

Compound 15e, 98.0+ % (HPLC)

031-21491

5 mg

for Cellbiology

371943-05-4

Ethanol

IC50 of PI3Kα: 2 nM; PI3Kβ: 16 nM;
PI3Kγ: 660 nM; PI3KC2β: 220 nM

Keep at 2 - 10°C

<Protein kinase inhibitor>

Permeable morpholino pyrimidine compound. A highly selective PI3Kα inhibitor.

Compound 401, 98.0+ % (HPLC)

033-21951

1 mg

for Cellbiology

168425-64-7

Methanol

IC50 of DNA-PK: 0.28 μM; mTOR: 5.3 μM;
ATM, ATR > 100 μM

Keep at -20°C.

039-21953

5 mg

<Protein kinase inhibitor>

Reversible and selective DNA-PK and mTOR inhibitor. It exhibits negligible affinity to PI3K, ATM and ATR. It has been known to inhibit mTOR-
dependent proliferation and induce apoptosis in TSC1-/- mouse embryo fibroblasts.

Deguelin

047-29211

5 mg

for Cellbiology

522-17-8

Acetone,
dichloromethane,
acetonitrile, DMSO

-

Keep at 2-10°C.

<Akt inhibitor>

Akt (Protein Kinase B; PKB) inhibitor. It inhibits proliferation of cells in the GM-2 stage of cell cycle. It induces apoptosis in the precancerous
and cancerated cell lines.

Dibucaine Hydrochloride, 98.0+ % (after drying)(Titration)

049-20011

1 g

for Biochemistry

61-12-1

Water, glacial acetic
acid, ethanol, acetone
and chloroform.

-

Keep at RT.

<Protein kinase inhibitor>

Lipophilic PKC inhibitor. Inhibits Na+ and K+-ATPase activities, too.

Dorsomorphin, 99.6% (HPLC, the initiall lot)

045-31221

1 mg

for Cellbiology

866405-64-3

Methanol

-

Keep at 2 - 10°C

041-31223

5 mg

<Protein kinase inhibitor>

Permeable pyrazolopyrimidine compound, which is potent, selective and reversible ATP-competitive inhibitor of AMPK (AMP-activated
protein kinasse). It has been shown to inhibit BMP signal strongly by inhibition of BMP type I receptors (ALK-2, ALK-3 and ALK- 6).

Dorsomorphin Dihydrochloride, 98.0+ % (HPLC)

047-31801

1 mg

for Cellbiology

1219168-18-9

Water

-

Keep at 2 - 10°C

043-31803

5 mg

<Protein kinase inhibitor>

This substance inhibits bone morphogenic factor (BMP) type I receptors (ALK2, ALK3 and ALK6). It has been shown to inhibit BMP signal
necessary for embryogenesis and accelerates important nerve differentiation from human pluripotential stem cells. It also functions as a
potent, selective and reversible ATP-competitive inhibitor of AMP-activating protein kinase (AMP-K).

Geldanamycin, from Streptomyces hygroscopicus, 95.0+ % (HPLC)

077-04571

100 μg

for Biochemistry

30562-34-6

Methanol

-

Keep at -20°C.

<Protein kinase inhibitor>

This product is an antitumor agent that has a benzoquinoid skeleton and has a pp60src tyrosine kynase inhibitory potency. Its
pharmacological action is more potent than that of herbimycin, which has a similar structure.

Genistein, 98.0+ % (HPLC)

073-05531

 20 mg

for Cellbiology

446-72-0

Ethanol

-

Keep at -20°C.

079-05533

100 mg

<Protein tyrosine kinase (PTK) inhibitor>

Isoflavone compound. Tyrosine kinase inhibitor by antagonizing against ATP. Known to inhibit the proliferation of various solid tumor cells
and induce the differentiation of the tumor cells.

Genistin, from Soybean; 98.0+ % (HPLC)

070-04681

 10 mg

for Biochemistry

529-59-9

Hot methanol

-

Keep at 2-10°C.

076-04683

100 mg

<Protein tyrosine kinase (PTK) inhibitor>

Soy extract isoflavone, or glucoside. Cancer-suppressing effects, antioxidant effects, and osteoporosis preventive effects have been
reported.

GF 109203X, 90.0+ % (HPLC)

079-03811

1 mg

for Cellbiology

133052-90-1

DMSO

IC50 of PKC: 10 nM

Keep at 2 - 10°C

<Protein kinase inhibitor / protein kinase C (PKC) inhibitor>

Potent and selective PKC inhibitor among bisindolylmaleimides, which have an inhibatory action on PKC. The structure is similar to that of
staurosporine.

Go 6983

070-05801

1 mg

for Cellbiology

133053-19-7

DMSO

IC50 of PKCα: 7 nM; PKCβ: 7 nM; PKCγ: 6 nM;
PKCδ: 10 nM; PKCζ: 60 nM; PKCμ: 20μM

Keep at -20°C.

<Protein kinase C (PKC) inhibitor>

Cell-permeable PKC inhibitor

GSK 269962A, 97.0+ % (HPLC)

070-05921

2 mg

for Cellbiology

850664-21-0

DMSO, acetonitrile

IC50 of ROCK-I: 1.6 nM; ROCK-II: 6 nM

Keep at 2 - 10°C

<Protein kinase inhibitor>

ROCK Inhibitor. Not available for sale in the USA due to patent.

GSK 429286A, 97.0+ % (HPLC)

073-05911

2 mg

for Cellbiology

850664-21-0

Ethanol, DMSO,
water

IC50 of ROCK: 14 nM

Keep at 2 - 10°C

<Protein kinase inhibitor>

ROCK inhibitor. It cancels out adrenaline-induced contraction of the aortic valve in rats and lowers the mean blood pressure in the arteries of
hypertensive rats.

H-1152 Dihydrochloride

088-09281

1 mg

for Cellbiology

871543-07-6

Water

IC50 of ROCK-II: 12 nM

Keep at -20°C.

<Protein kinase inhibitor>

ROCK inhibitor. Its inhibitory activity is more potent than that of Y-27632. It exhibits weak affinity to other serine/threonine kinases.

Herbimycin A, 98.0+ % (HPLC)

085-06491

1 mg

for Biochemistry

70563-58-5

Methanol, DMSO

-

Keep at 2-10°C.

<Protein tyrosine kinase (PTK) inhibitor>

Tyrosine kinase inhibitor by binding to the SH group of cysteine in oncogene src. It also inhibits transformation activity of oncogenes (src,
yes, fps, ros, abl, erbB) that have tyrosine kinase activity. It also has the unique ability to restore RSVts-NRK cells to their normal form.

Hypericin, from Hypericum perforatum

086-07761

1 mg

for Biochemistry

548-04-9

Water-THF

-

Keep at 2 - 10°C

082-07763

5 mg

<Protein kinase inhibitor / PKC inhibitor>

Inhibitor of PKC, insulin receptor, EGF receptor, casein kinase II, and thyrosine kinase activity of MAPK. It also exhibits antivirus and
antiretrovirus activities.

IPA-3, 97.0+ % (HPLC)

093-06231

5 mg

for Cellbiology

42521-82-4

DMSO, acetonitrile

PAK1: IC50 = 2.5 μM

Keep at 2 - 10°C

<Protein kinase inhibitor>

p21 activation kinase (PAK) inhibitor, which binds to the regulatory domain of PAK and accelerates inactivation of PAKs structure. Shows
high selectivity to PAK1 in particular. PAK1 involves in tumor formation and metastasis.

K-252a

113-00561

 50 μg

for Biochemistry

97161-97-2

Ethyl acetate

-

Keep at -20°C.

119-00563

100 μg

117-00564

250 μg

<Protein kinase inhibitor / PKC inhibitor>

Selective inhibitor of PKA (cyclic AMP-dependent protein kinase), PKC (phospholipid-dependent protein kinase) and PKG (cyclic GMP-
dependent protein kinase).

K-252b

110-00571

 50 μg

for Biochemistry

99570-78-2

Methanol

-

Keep at -20°C.

114-00574

250 μg

<Protein kinase inhibitor / PKC inhibitor>

Selective inhibitor of PKA (cyclic AMP-dependent protein kinase), PKC (phospholipid-dependent protein kinase) and PKG (cyclic GMP-
dependent protein kinase).

Kenpaullone

110-00831

1 mg

for Cellbiology

142273-20-9

DMSO

-

Keep at -20°C.

116-00833

5 mg

<CDK Inhibitor>

Potent GSK-3β and CDK inhibitor. Inhibits antagonistically ATP binding. Reported to be substitutable for Klf4, one of the 4 Yamanaka
factors (Oct3/4, Klf4, Sox2, c-Myc), in iPS cell production. Also reported to improve reprogramming efficiency if added upon the introduction
of 4 Yamanaka factors.

Ki 8751, 96.0+ % (HPLC)

112-00891

5 mg

for Cellbiology

228559-41-9

DMSO

IC50 = 0.9 nM

Keep at -20°C.

<Protein kinase inhibitor>

Potent and selective VEGFR-2 tyrosine kinase inhibito.

KN-62

118-00631

1 mg

for Biochemistry

127191-97-3

Methanol, DMSO

Ca2+ / calmodulin-dependent protein
kinase II (in rat brain): IC50 = 0.3 μM

Keep at 2-10°C.

114-00633

5 mg

<Kinase inhibitor / Calmodulin antagonist>

Selective inhibitor of Ca calmodulin-dependent protein kinase II in the rat brain. It inhibits the proliferation of K562 cells (1 μM).

KN-93

115-00641

1 mg

for Biochemistry

139298-40-1

Methanol

Ca2+ / calmodulin-dependent protein
kinase II (in rat brain): IC50 = 2.0 μM

Keep at 2-10°C.

111-00643

5 mg

<PKC inhibitor / Calmodulin antagonist>

Selective inhibitor of Ca calmodulin-dependent protein kinase II in the rat brain. Inhibits insulin release from isolated islands of Langerhans
caused by glucose induction and forskolin stimulation. It induces stoppage of the cell cycle in theG1 phase and apoptosis in NIH3T3 cells.

KN-93, Water-Soluble

114-00731

1 mg

for Cellbiology

-

Water

-

Keep at -20°C.

<PKC inhibitor>

Selective inhibitor of Ca calmodulin-dependent protein kinase II in the rat brain. Inhibits insulin release from isolated islands of Langerhans
caused by glucose induction and forskolin stimulation. It induces stoppage of the cell cycle in theG1 phase and apoptosis in NIH3T3 cells.

KT 5720

117-00581

 50 μg

for Biochemistry

108068-98-0

Methanol

-

Keep at -20°C.

113-00583

100 μg

111-00584

250 μg

<Protein kinase inhibitor>

K252a derivative and membrane permeable PKA (cyclic AMP-dependent protein kinase) inhibitor

KT 5823

114-00591

 50 μg

for Biochemistry

126643-37-6

Ethyl acetate,
methanol

-

Keep at -20°C.

110-00593

100 μg

118-00594

250 μg

<PKC inhibitor>

Cell-permeable PKC inhibitor

KU 0063794, 98.0+ % (HPLC)

115-00881

5 mg

for Cellbiology

938440-64-3

Acetone,
dichloromethane,
acetonitrile, DMSO

IC50 of mTOR1: 10 nM; mTOR2: 10 nM.

Keep at 2-10°C.

<Akt inhibitor>

Selective mTOR (mammalian target of rapamycin) inhibitor. Shows no inhibitory activity against 76 types of protein kinases including PI3K
even at 1,000-fold concentration.

LDN 193189 Hydrochloride, 98.0+ % (HPLC)

124-06011

2 mg

for Cellbiology

1062368-62-0

Water

IC50 of ALK2: 5 nM; ALK3: 30 nM.

Keep at 2 - 10°C

<Protein kinase inhibitor>

This product inhibits ALK2 and ALK3, which are BMP type I receptors, and consequently inhibits phosphorylation of Smad1, Smad5 and
Smad8.

LY 294002, 97.0+%(HPLC)

129-04861

 5 mg

for Biochemistry

154447-36-6

Ethanol, acetone

IC50 of PI3-kinase: 1.4 μM;

Histamine secretion by PBL-2H3: 5 μM.

Keep at 2-10°C.

125-04863

10 mg

123-04864

25 mg

<Akt inhibitor>

Highly cell-permeable, specific phosphatidylinositol 3-kinase (PI3-kinase) inhibitor. It inhibits the proliferation of rabbit aorta smooth muscle
cells without inducing apoptosis. It is also reported to inhibit histamine secretion by RBL-2H3 cells.

Lys-Lys-Lys-Leu-Arg-Arg-Gln-Glu-Ala-Phe-Asp-Ala-Tyr

331-43741

0.5 mg

Peptide Institute

(4374-v)

-

Water

IC50 = 4.1 nM

Keep at -20°C.

<Protein kinase inhibitor>

Inhibitor of calmodulin-dependent protein kinase II.

3-Methyladenine

131-17671

100 mg

for Biochemistry

5142-23-4

 -

-

Keep at -20°C.

137-17673

1 g

<PI3 kinase inhibitor>

This product prevents downstream mTOR kinase activity degradation by inhibition of PI3-kinase , which in turn suppresses autophagy.

NSC 693868, 98.0+ % (HPLC)

140-08891

5 mg

for Cellbiology

40254-90-8

DMSO

-

Keep at 2 - 10°C

<Protein kinase inhibitor>

Selective inhibitor of GSK-3β and CDK5.

NU 7026, 97.0+ %

145-08841

5 mg

for Cellbiology

154447-35-5

DMSO

IC50 of DNA-PK: 0.23 μM; PI3K: 13.0 μM;
ATM, ATR >100 μM

Keep at 2 - 10°C

<Protein kinase inhibitor>

ATP-competitive inhibitor of the protein kinase DNA-PK (DNA-dependent protein kinase).

NU 7441, 98.0+ % (HPLC)

143-09001

1 mg

for Cellbiology

503468-95-9

Methanol

IC50 of DNA-PK: 14 μM; mTOR: 1.7 μM;
PI3K: 13.0 μM; ATM, ATR >100 μM

Keep at -20°C.

149-09003

5 mg

<Protein kinase inhibitor>

Potent, reversible and selective inhibitor of DNA-PK (DNA-dependent protein kinase) and mTOR. Has little affinity with PI3K, ATM, and ATR.
Known to inhibit mTOR-dependent proliferation and induce apoptosis in TSC1-/- mouse embryonic fibroblasts.

Olomoucine, 97+ % (TLC)

157-01901

5 mg

for Biochemistry

101622-51-9

DMSO

-

Keep at -20°C.

<CDK Inhibitor / MAPK inhibitor>

It inhibits p34cdc/cyclin B, p33cdk2/cyclin A, p33cdk2/cyclin E, cerebral p33cdk5/p35 and erk1/MAPK, and it has been reported to inhibit in vitro the
transition of the G2/M phase in the oocytes of starfish, and the transition of the G1/S phase in the mesophyll protoplasts of petunia.

PD-98059, 95+ % (TLC)

169-19211

5 mg

for Biochemistry

167869-21-8

Ethanol, acetone

-

Keep at -20°C.

<Protein kinase inhibitor/ MAPK inhibitor>

MAPK-1 inhibitor. This product has been reported to inhibit MAPK activation by insulin and block completely the increase in cell growth and
MAP activity induced by leptin (obesity regulating hormone). The resting cell pretreated with PD-98059 has been demonstrated to inhibit a
great deal the expression of the advance early genes c-fos and eggr-1 induced by a peroxisome proliferative agent.

PD 173074

166-24351

5 mg

for Cellbiology

219580-11-7

Methanol

- 

Keep at 2-10°C.

<PTK inhibitor>

ATP competitive type FGF receptor inhibitor. The FGF signaling pathway is associated with spontaneous proliferation of stem cells in a host
of systems.

PD 184352, 98.0+ % (HPLC)

169-25181

5 mg

for Cellbiology

212631-79-3

Methanol, DMSO

-

Keep at 2-10°C.

<MAPK Inhibitor>

Poteent and selective inhibitor of MEK1. Recent studies showed that culturing ES cells in a medium containing CHIR99021, SU5402,
PD184352 allows for highly-efficient suppression of differentiation.

PD 0325901

162-25291

 5 mg

for Cellbiology

391210-10-9

Methanol, DMSO

IC50 of MEK: 0.33 nM

Keep at -20°C.

168-25293

25 mg

<MAPK Inhibitor>

MAPK inhibitor with potent antitumor activity. It induces phosphorylation of MAPK, inhibition of its activation and inhibition of tumor cell
proliferation. PD0325901 inhibits MAPK activity without adverse reactions. Addition of this product and CHIR99021 to a culture medium
results in efficient culture of mouse ES cells.

Phloretin, 98.0+ % (HPLC)

160-17781

250 mg

for Biochemistry

60-82-2

Methanol

IC50 = 16 μM

Keep at 2 - 10°C

<PKC inhibitor>

The aglycone moiety of phlorizin, a specific inhibitor of the sugar active transport system, which is actually responsible for the inhibitory
action of phlorizin.

When used alone, phloretin has been reported to be less effective for the active transport system while it is known to be more inhibitory than
phlorizin to the carrier transport system, suggesting a difference in the mode of action according to structure.

It is also useful as means for the study of the kinetics and regulatory mechanisms of PKC as a non-specific inhibitor of PKC.

PI-103, 98.0+ % (HPLC)

163-24241

 1 mg

for Cellbiology

371935-74-9

DMSO

-

Keep at -20°C.

169-24243

10 mg

<Akt inhibitor>

Potent, cell-permeable and ATP-competitive inhibitor of DNA-PK, PI-3K, and mTOR with selectivity for a wide range of lipids and protein
kinases. Reported to inhibit PIP3 production, insulin signal transduction, and Akt phosphorylation, suppress cell proliferation, and induce cell
death.

Piceatannol

169-21661

10 mg

for Cellbiology

10083-24-6

Ethanol

-

Keep at 2 - 10°C

<Protein kinase inhibitor / PTK inhibitor>

Selective inhibitor of non-reception type tyrosine kinase Syk. An activator of human deacetylase class III (SIrt1).

PIK-75 Hydrochloride, 98.0+ % (HPLC)

162-24451

5 mg

for Cellbiology

-

Water-methanol

IC50 of PI3Kα: 0.3 nM; PI3Kβ: 850 nM;
PI3Kγ: 40 nM; PI3K C2β: 100 nM

Keep at 2 - 10°C

<Protein kinase inhibitor>

Cell-permeable imidazopyridine compound, which is a selective inhibitor of PI3Kα.

PKC 412, 96.0+ % (HPLC)

164-25751

 1 mg

for Cellbiology

120685-11-2

-

-

Keep at -20°C.

160-25753

10 mg

<Protein kinase inhibitor>

Wide range of kinase inhibitor. Inhibits PKC, PDFRβ, VEGFR2, Syk, PKCη, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1,EGFR, etc.

PP 2, 94.0+ % (HPLC)  

166-20331

1 mg

for Biochemistry

172889-27-9

Methanol, DMSO

-

Keep at -20°C.

<PTK inhibitor>

Src family tyrosine kinase inhibitor.

PP 3, 94.0+ % (HPLC)

163-20341

1 mg

for Biochemistry

5334-30-5

Methanol

-

Keep at -20°C.

<PTK inhibitor>

EGF receptor type tyrosine kinase inhibitor

PP 242, 98.0+ % (HPLC)

165-24441

5 mg

for Cellbiology

1092351-67-1

DMSO

IC50 of mTOR: 8 nM; PI3Kα: 2 μM; PI3Kβ:
2.2 μM; PI3Kγ: 1.3 μM; PI3Kδ: 0.1 μM

Keep at 2-10°C.

<Akt inhibitor>

Potent and selective mTOR (mammalian target of rapamycin) inhibitor

Quercetin Dihydrate

171-00404

100 mg

Practical Grade

6151-25-3

Ethanol, acetone

-

Keep at RT.

177-00401

1 g

173-00403

10 g

<Akt inhibitor>

Yellow flavonoid. Has antioxidant and anti-tumor effects. Its fat absorption inhibitory effect is particularly strong compared with other
polyphenols, and it aids in eliminating the body fat. Boosts the fat metabolism in the liver, increases fat combustion, and inhibits fat
absorption by binding to fat in the digestive tract. Also said to reduce the inflammation in pollinosis.

Rac1 Inhibitor, 98.0+ % (HPLC)

180-02491

5 mg

for Cellbiology

-

Water

-

Keep at 2-10°C.

<MAPK Inhibitor>

Selective inhibitor of Rac1-GEF interaction. Specifically inhibits Rac1 activity by inhibiting the interactions between Rac1 and Rac-specific
GEFs (guanine nucleotide exchange factors), TrioN and Tiam1.

Radicicol, 97.0+ % (HPLC)

183-01901

1 mg

for Cellbiology

12772-57-5

Ethanol, methanol,
DMSO

-

Keep at -20°C.

<PTK inhibitor>

Macrocyclic lactone antifungal antibiotic with antimalarial activity. It inhibits a heat shock protein 90 (HSP90) and protein tyrosine kinase.

Rapamycin (mixture of isomers)

184-02531

 1 mg

for Cellbiology

53123-88-9

-

-

Keep at -20°C.

180-02533

10 mg

188-02534

50 mg

<Protein kinase inhibitor>

Macrolide immunosuppressive agent. A structural analog of FK506 that binds to FK506 binding proteins (FKBPs) but does not inhibit
calcineurin activity. The rapamycin-FKBP complex inhibits the signal from IL-2 by inhibiting the kinase activity of mTOR. Inhibits G1-to-S
phase transition of the cell cycle.

RG-14620

188-02811

10 mg

for Cellbiology

136831-49-7

-

IC50 = 3μM

Keep at -20°C.

184-02813

50 mg

<Protein kinase inhibitor>

EGFR tyrosine kinase inhibitor

Ro 31-8220 Methanesulfonate

186-02591

1 mg

for Cellbiology

138489-18-6

Ethanol

IC50 of PKCα: 5 nM; PKCβI: 24 nM;

PKCβII: 14 nM; PKCγ: 27 nM; PKCε: 24 nM;
PKA: 0.9 μM; CaM kinase II: 17 μM

Keep at 2-10°C.

<PKC inhibitor>

A structural analog of staurosporine. Potent, cell-permeable PKC inhibitor. Its selectivity for PKAs and CaM kinase II is low, and it also has
inhibiting effects on glycogen synthase kinase 3 (GSK3) and voltage-dependent Na channels.

Roscovitine, 98.0+ % (HPLC)

182-01591

 1 mg

for Biochemistry

186692-46-6

DMSO, ethanol,
acetone

-

Keep at -20°C.

188-01593

10 mg

<CDK inhibitor>

Olomoucine analog and CDK2 and CDK5 inhibitor. In Alzheimer's disease, it is believed to be associated with hyperphosphorylated tau.

SB 202190

193-13531

1 mg

for Cellbiology

152121-30-7

Methanol

-

Keep at -20°C.

<MAPK Inhibitor>

Potent and selective inhibitor of the p38α and β isoforms of p38 MAPK family. Shows membrane permeability. It has no effect on ERK and
JNK MAPK.

SB 203580, 98.0+ % (HPLC)

199-16551

 1 mg

for Cellbiology

152121-47-6

DMSO, methanol

IC50 of SAPK2a / p38: 50 nM;
SAPK2b / p38β2: 50 nM

Keep at -20°C.

195-16553

10 mg

<Protein kinase inhibitor / MAPK inhibitor>

Specific MAPK p38α and p38β inhibitor. Also used to separate and maintain embryonic stem cells (ES cells).

SB 203580 Hydrochloride, 98.0+ % (HPLC)

198-16761

1 mg

for Cellbiology

869185-85-3

Water

IC50 of p38α (in vitro): 34 nM;
(in vivo): 600 nM

Keep at -20°C.

<MAPK Inhibitor>

Specific MAPK p38α and p38β inhibitor. Also used to separate and maintain embryonic stem cells (ES cells).

SB 415286, 98.0+ % (HPLC)

197-15751

5 mg

for Cellbiology

264218-23-7

DMSO

-

Keep at -20°C.

<Protein kinase inhibitor>

Potent, cell-permeable, and selective GSK-3 inhibitor. GSK-3β inhibitors are used in a variety of stem cell research including ES cells and
iPS cells. Reduces the cell death of cerebellar granule neurons in vivo. Also increases cytoplasmic β-catenin concentration and inhibits
GSK-3-dependent tau phosphorylation. Also reported to stimulate glycogen synthesis and gene transcription and have protective effects on
the heart and nerves.

SB 431542, 98.0+ % (HPLC)

192-16541

 5 mg

for Cell Culture

331752-47-7

DMSO

IC50 of ALK = 7 nM

Keep at -20°C.

198-16543

25 mg

<Protein kinase inhibitor>

Selective inhibitor of activin receptor-like kinase (ALK) 4, 5 and 7 (the TGF-β type I receptor).

Promotes proliferation, differentiation and sheet formation of endothelial cells of ES cell origin. Can be able to grow dramatically efficiency
reprogramming to Human iPS Cells when used with Thiazovivin and PD0325901. It also promotes the speed.

SP 600125, 98.0+ % (HPLC)

197-16591

 5 mg

for Cellbiology

129-56-6

Acetone, DMSO

IC50 of JNK1: 40 nM; JNK2: 40 nM;
JNK3: 90 nM

Keep at -20°C.

193-16593

25 mg

<MAP kinase inhibitor>

MAPK inhibitor and potent ATP-competitive inhibitor of the c-Jun N-terminal kinase (JNK) subfamily.

Its selectivity to JNK exceeds 20 times that of ERK and p38 MAPK. It inhibits c-Jun phosphorylation and the expression of inflammatory
genes such as COX-2, LI-2, IFN-γ, and TNF-α. It is neuroprotective in vivo.

D-erythro-Sphingosine, 99+% (TLC)

192-11161

25 mg

for Biochemistry

123-78-4

Methanol-
chloroform mixture

IC50 of PKC: 1 - 3 μM

Keep at -20°C.

<Protein kinase inhibitor / PTK inhibitor>

Selective PKC inhibitot. It exhibit inhibitory action competitively to diacylglycerol, phorbol dibutyrate and Ca2+. It does not affect the
activities of MLCK and PKA. It has also been reported to induce apoptosis in human myelocytic leukemia cells, HL-60.

SR 3677 Hydrochloride, 98.0+ % (HPLC)

195-16151

2 mg

for Cellbiology

1072959-67-1

Water, DMSO

IC50 of ROCK-I: 56 nM, ROCK-II: 3 nM

Keep at RT.

<Protein kinase inhibitor>

Potent ROCK inhibitor

Staurosporine, 95.0+ % (HPLC)

197-10251

100 μg

for Biochemistry

62996-74-1

DMSO

IC50 of PKC: 2.7 nM; PKA: 8.2 nM;
p60v-src tyrosine kinase: 6.4 nM

Keep at -20°C.

193-10253

500 μg

<PKC inhibitor / CDK inhibitor>

A microbial alkaloid and extremely potent inhibitor of protein kinase Cs (PKCs). Also has comparable inhibitory actions on cAMP-dependent
protein kinases (PKAs) and p60v-src tyrosine kinase, the product of an oncogene src.

Stellettamide A Trifluoroacetate, 95.0+ % (HPLC)

193-11831

100 μg

for Biochemistry

129744-24-7

Methanol

-

Keep at -20°C.

<PKC inhibitor>

Substance isolated and extracted from sponge (Stelletta sponge). It inhibits calmodulin.

SU 4312, 97.0+ % (HPLC)

190-15861

5 mg

for Cellbiology

-

Ethanol

Ki: unactivated form: 0.04 μM;
activated form: 4 μM

Keep at -20°C.

<Protein kinase inhibitor / Akt inhibitor>

VEGFR2 tyrosine kinase inhibitor. Also Inhibits angiogenesis in tumors.

SU 5402, 95.0+ % (HPLC)

193-16071

1 mg

for Cellbiology

215543-92-3

DMSO

-

Keep at -20°C.

<PTK inhibitor>

Tyrosine kinase inhibitor in fibroblast growth factor receptor 1 (FGFR1). It also inhibits phosphorylation of ERK1 and ERK2 induced by aFGF.
A recent study has demonstrated inhibition of differentiation at a high efficiency by incubating ES cells in a medium containing CHIR99021,
SU5402 and PD184352.

SU 5416, 97.0+ % (HPLC)

196-15841

5 mg

for Cellbiology

204005-46-9

Ethanol

IC50 of VEGFR2: 1.3 μM; FGFR1: 4.2 μM;
PDGFRβ: 37.9 μM

Keep at -20°C.

<Protein kinase inhibitor / Akt inhibitor>

VEGFR2 tyrosine kinase inhibitor. Also Inhibits angiogenesis in tumors.

SU 6668, 98.0+ % (HPLC)

193-15851

5 mg

for Cellbiology

252916-29-3

Ethanol

IC50 of VEGFR2: 3.9 μM; FGFR1: 3.8 μM;
PDGFRβ: 0.10 μM

Keep at 2 - 10°C

<Protein kinase inhibitor>

VEGFR2 tyrosine kinase inhibitor

SU 11274, 95.0+ % (HPLC)

198-17121

 5 mg

for Cellbiology

658084-23-2

-

IC50 of c-MET tyrosine kinase: 10 nM;
VEGFR1/2 tyrosine kinase: 0.8 mM;
PDGFR: 19.4 mM

Keep at -20°C.

194-17123

25 mg

<Protein kinase inhibitor>

Selective inhibitor of c-MET tyrosine kinase.

Tamoxifen Citrate, 98.0+ % (Ti)

209-14361

250 mg

for Biochemistry

54965-24-1

Ethanol

IC50 of PKC: 2.7 nM; PKA: 8.2 nM;
p60v-src tyrosine kinase: 6.4 nM

Keep at 2-10°C.

205-14363

1 g

203-14364

5 g

207-14362

25 g

<PKC inhibitor>

Estrogen analog, which is used as a drug used for prophylactic therapy of breast cancer, is known to selectively bind to estrogen receptors
and is also called SERM (selective estrogen receptor modifier). It is considered to be deeply associated with diseases such as breast cancer
and osteoporosis.

Triciribine, 95.0+ % (HPLC)

206-19371

5 mg

for Cellbiology

35943-35-2

-

IC50 of AKT kinase: 150 nM

Keep at -20°C.

<Protein kinase inhibitor>

Triciribine is inhibitor of AKT1/2/3 kinase and DNA synthesis inhibitor.

TWS 119, 90.0+ % (HPLC)

206-17671

1 mg

for Cellbiology

601514-19-6

Methanol

-

Keep at 2 - 10°C

202-17673

5 mg

<Protein kinase inhibitor>

Acts as a potent and selective inhibitor of GSK-3β. Also reported to selectively induce neuronal differentiation in murine embryonic stem
cells.

Tyrphostin A25, 95.0+ % (HPLC)

204-19311

10 mg

for Cellbiology

118409-58-8

-

IC50: 3 μM

Keep at -20°C.

200-19313

50 mg

<Protein kinase inhibitor>

EGFR tyrosine kinase inhibitor

U 0126 (mixture of isomers), 95.0+ % (HPLC)

211-01051

5 mg

for Biochemistry

109511-58-2

Acetonitrile, ethanol

-

Keep at -20°C.

<MAP kinase inhibitor>

MAPK inhibitor used for signal transduction studies.

W-5 Hydrochloride

236-01721

 5 mg

for Biochemistry

61714-25-8

Methanol, water

IC50 of PDE: 240 μM; MLCK: 230 μM

Keep at -20°C.

232-01723

25 mg

<PKC inhibitor / Calmodulin antagonist>

A naphthalenesulfonate amide calmodulin antagonist to inhibit Ca2+/calmodulin-dependent phosphodiesterase (PDE) and myosin light chain
kinase (MLCK). However, compared to W-7, its action as a calmodulin antagonist is low, and the product is mainly used as a negative
control of W-7.

W-7 Hydrochloride

233-01731

  5 mg

for Biochemistry

61714-27-0

Methanol, water

IC50 of PDE: 28 μM; MLCK: 51 μM

Keep at -20°C.

239-01733

 50 mg

237-01734

250 mg

<Protein kinase inhibitor / Calmodulin antagonist>

A naphthalenesulfonate amide calmodulin antagonist to inhibit Ca2+/calmodulin-dependent phosphodiesterase and myosin light chain kinase.

(+)-Wortmannin, 97.0+ % (HPLC)

230-02341

 2 mg

for Cellbiology

19545-26-7

Ethanol

-

Keep at -20°C.

236-02343

10 mg

<Akt inhibitor>

Has selective and irreversible inhibitory actions on myosin light chain kinases, a type of protein kinase that regulates smooth muscle
contraction etc., and concentration-dependent and irreversible inhibitory actions on phosphatidylinositol 3-kinases, which are involved in
phosphatidylinositol metabolism, one of the intracellular signal transduction mechanisms.

Y-27632, 98.0+ % (HPLC)

257-00511

 1 mg

for Cellbiology

146986-50-7

Water

p160ROCK (Ki = 140 nM)

Keep at -20°C.

253-00513

 5 mg

251-00514

25 mg

<Protein kinase inhibitor>

Selective and potent ROCK inhibitor. It inhibits contraction of the vascular smooth muscle, infiltration of cancer cells, and regulation of cell
differentiation caused by a signal transduction system of ROCK. Enhances survival rate after cryopreservation and cloning efficiency of
human ES and iPS cells.

5 mmol/L Y-27632 Solution

253-00591

300 μL

for Cell Culture

331752-47-7

-

-

Keep at -20°C.

<Protein kinase inhibitor>

5 mmol/L Y-27632 in aqueous soution.

indexpage top

2. Protein Phosphatase Inhibitors

Product Name

Wako Cat. No.

Pkg. Size

Grade/Manufacturer

CAS No.

Soluble in

IC50

Storage Condition

Summary

Calyculin A, 95.0+ % (HPLC)

038-14453

 10 μg

for Biochemistry

101932-71-2

Methanol, ethanol,
DMSO

IC of PP2A: 3 nM; smooth muscle: 5 nM;

smooth muscle endogenous: 1 nM

Keep at -20°C.

032-14451

100 μg

Contracts the smooth muscle regardless of the presence of external calcium, with its effects being approximately 100 times more potent
than okadaic acid. A variety of actions have been confirmed, such as equally-potent inhibition of type 1 and 2A phosphatase activities and
promotion of protein phosphorylation.

Cantharidin

036-20461

 25 mg

for Cellbiology

56-25-7

Acetone

IC50 of PP2A: 40 nM; PPA: 473 nM

Keep at 2-10°C.

032-20463

100 mg

030-20464

500 mg

Potent and selective protein phosphatase 2A inhibitor. Also inhibits protein phosphatase 1 at high concentrations.

Cyclosporin A, 97.0+ % (HPLC)

031-18963

 50 mg

for Cellbiology

59865-13-3

Methanol, ethanol,
acetone, ether,
chloroform

-

Keep at 2-10°C.

035-18961

200 mg

It is a representative immunosuppressant used for prevention of rejection reaction at the time of organ transplantation and it binds to the
intracellular receptor in T lymphocytes inhibiting IL-2 and IFN-γ transcription (calcineurin inhibition). Consequently, it inhibits activation and
proliferation of helper T cells contributing to immune reaction.

Fostriecin Sodium Salt

065-05051

10 μg

for Cellbiology

87860-39-7

Ethanol, water

IC50 of PP1: 131 nM; PP2A: 3.2 nM

Keep at -20°C.

An antibiotic with anti-tumor activity isolated from Streptomyces pulveraceous (subspecies fostreus). Binds near the active center of the
catalytic subunit of PP2A and inhibits substrate dephosphorylation. Does not affect PP2B enzyme activity but shows inhibitory action on
PP1 as well at high concentrations.

RK-682, 95.0+ % (HPLC)

185-01341

1 mg

for Biochemistry

-

Ethanol, acetone

IC50 of CD45: 54 μM; VHR: 2.0 μM

Keep at RT.

Specific tyrosine phosphatase inhibitor, which inhibits dephosphorylation of CD45 or VHR, protein-tyrosine phosphatase (PTPase), and
regulates the cell cycle from G1 to S period.

Tautomycin

209-12041

100 μg

for Biochemistry

109946-35-2

Chloroform,
ethanol, methanol

IC50 of PP2A, PP1 (smooth muscle):
32 nM; PP1 (skeletal muscle): 22 nM;
Smooth muscle endofenous: 6 nM

Keep at -20°C.

Protein phosphatase inhibitor and antifungal antibiotic produced from Streptomyces spiroverticillatus.

Disodium β-Glycerophosphate Pentahydrate, 95.0+ % (Titration)

046-31251

 50 g

for Cellbiology

13408-09-8

Water: 1 g/20 mL

-

Keep at 2-10°C.

042-31253

250 g

Has a structure of phosphorylated glycerol and in animal tissues is released into the blood with the breakdown of triglycerides in the liver.
Also produced as a glycolytic intermediate.

Levamisole Hydrochloride, 98.0+ % (Titration)

123-04641

10 g

for Biochemistry

16595-80-5

Water: 210 g/L

(20°C)

-

Keep at RT.

Powder type of alkaline phosphatase inhibitor. It promotes the maturation of T lymphocytes and increases cellular immune responses.

indexpage top

3. Inhibitor Cocktail Sets

Product Name

Wako Cat. No.

Pkg. Size

Grade/Manufacturer

CAS No.

Soluble in

IC50

Storage Condition

Summary

Phosphatase Inhibitor Cocktail Solution I (×100)

167-24381

1 mL

for Cellbiology

-

-

-

Keep at 2-10°C.

5 phosphatase inhibitor mixture [Inhibition Target] serine/threonine phosphatases, tyrosine phosphatases, and dual-specificity phosphatases
[Composition] sodium fluoride, sodium orthovanadate, sodium pyrophosphate, β-glycerophosphate, and sodium molybdate

Phosphatase Inhibitor Cocktail Solution II (×100)

160-24371

1 mL

for Cellbiology

-

-

-

Keep at 2-10°C.

5 phosphatase inhibitor mixture [Inhibition Target] acid phosphatases; alkaline phosphatases; tyrosine phosphatases

[Composition] sodium fluoride, sodium tartrate, sodium orthovanadate, imidazole, and sodium molybdate

Protease Inhibitor Cocktail Set I, Animal-derived-free (for general use) (x 100), Lyophilized

165-26021

for 1 mL

for Cellbiology

-

-

-

Keep at -20°C.

161-26023

for 1 mL x 5

5 inhibitor mixture solution. It replaces aprotinin from bovine lung with recombinant aprotinin produced with no animal by-products.

[Inhibition Target] a wide variety of proteases and esterases.

Protease Inhibitor Cocktail Set III, DMSO Solution (EDTA free) (x 100)

163-26061

1 mL

for Cellbiology

-

-

-

Keep at -20°C.

169-26063

1 mL x 5

6 inhibitor mixture solution being suitable for experiments targeted on metal-binding proteins in mammalian cells, tissue extracts, and
bacterial extracts. It does not contain EDTA or other metalloproteinase inhibitors.

[Inhibition Target] a wide range of proteases including aminopeptidases.

Protease Inhibitor Cocktail Set III, DMSO Solution, Animal-derived-free (EDTA free) (×100)

160-26071

1 mL

for Cellbiology

-

-

-

Keep at -20°C.

166-26073

1 mL x 5

6 inhibitor mixture solution being suitable for experiments targeted on metal-binding proteins in mammalian cells, tissue extracts, and
bacterial extracts. It inhibits a wide range of proteases including aminopeptidases. It does not contain EDTA or other metalloproteinase
inhibitors. It replaces aprotinin from bovine lung with recombinant aprotinin produced with no animal by-products.

Protease Inhibitor Cocktail Set IV, DMSO Solution (for Fungal and Yeast) (×100)

167-26081

1 mL

for Cellbiology

-

-

-

Keep at -20°C.

163-26083

1 mL x 5

4 inhibitor mixture DMSO solution, being suitable for use in mold and yeast extracts.

[Inhibition Target] serin proteases, cystein proteases, metalloproteases, asparatic proteases.

Protease Inhibitor Cocktail Set V (EDTA free) (×100), Lyophilized

162-26031

for 1 mL

for Cellbiology

-

-

-

Keep at -20°C.

168-26033

for 1 mL x 5

4 inhibitor mixture solution, being suitable for experiments targeted on metal-binding proteins and recombinant proteins.

In addition, also useful for metal-affinity column chromatography.

[Inhibition Target] serin proteases, cystein proteases, metalloproteases, asparatic proteases.

Protease Inhibitor Cocktail Set VI, DMSO Solution (for Plant) (×100)

164-26091

1 mL

for Cellbiology

-

-

-

Keep at -20°C.

160-26093

1 mL x 5

6 inhibitor mixture solution, being suitable for plant extracts.

[Inhibition Target] serin proteases, cystein proteases, trypsin-like proteases, aminopeptidase B, leucine aminopeptidase, asparatic proteases,
metalloproteases.

Protease Inhibitor Cocktail Set VII, DMSO Solution (for Histidine-tagged Protein) (× 100)

167-26101

1 mL

for Cellbiology

-

-

-

Keep at -20°C.

163-26103

1 mL x 5

EDTA-free 5 inhibitor mixture solution, being suitable for purification of histidine-tagged proteins.

[Inhibition Target] serin proteases, cystein proteases, aminopeptidase B, leucine aminopeptidase, asparatic proteases, metalloproteases.

indexpage top

4. Calcium Signaling related Inhibitors

Product Name

Wako Cat. No.

Pkg. Size

Grade/Manufacturer

CAS No.

Soluble in

IC50

Storage Condition

Summary

Alendronate Sodium Salt Trihydrate, 97.0+ % (HPLC)

012-22661

100 mg

for Pharmacology
Research

121268-17-5

Water

IC50 = 10 μM

Keep at -20°C.

018-22663

500 mg

<Calcium metabolism regulator>

This product is a bisphosphonate compound that is selectively distributed in the calcified bone surface to which the osteoclasts are attached.
It is released under an acid environment created by the osteoclasts, taken in the cells, and inhibits the bone resorption activity. The inhibition
of the bone resorption is considered to be caused by apoptosis induction effect of the osteoclasts and direct suppression of bone resorption
of the osteoclasts.

(-)-Blebbistatin, 98.0+ % (HPLC)

021-17041

1 mg

for Cellbiology

856925-71-8

DMSO (5 mg/mL)

-

Keep at -20°C.

027-17043

5 mg

<Calcium ATPase Inhibitors>

Specific inhibitor of myosin II. It inhibits contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly in the
vertebrate cell divisions. It has been reported to block blebbing and apoptosis and increases the colony forming rate when human ES cells
are dispersed to single cells from a colony.

Calpain Inhibitor 2, 95.0+ % (HPLC)

038-19811

10 mg

for Cellbiology

110115-07-6

Ethanol, methanol

-

Keep at -20°C.

<Calpain inhibitors>

This product inhibits neutral cysteine proteinases such as calpain 1, calpain 2, cathepsin B and cathepsin L. It is also a weak inhibitor of
proteasomes.

Chlorpromazine Hydrochloride, 99.0+ % (Titration)

033-10581

10 g

for Biochemistry

69-09-0

Water, ethanol

IC50 = 25 μM

Keep below 25°C.

<Calmodulin antagonists>

Chlorpromazine Hydrochloride is a phenothiazine neuroleptic which induces tranquilization, analgesia, lowering of body temperature by
inhibiting the hypothalamic thermoregulatory mechanism, antiemesis by inhibiting CTZ of the medulla oblongata, inhibition of conditioned
avoidance response, and hypnosis, as well as an antidopaminergic. This reagent potently blocks α-adrenergic receptors. Its mode of action
in the biogenic system is inhibition of calmodulin, similar to trifluoperazine.

Cyclopiazonic Acid, 98.0+ % (HPLC)

030-17171

5 mg

for Biochemistry

18172-33-3

Methanol

IC50 of Ca2+: 0.2 μM; ATPase: 0.35 μM

Keep at -20°C.

<Calcium ATPase Inhibitors>

Mycotoxin (fungal toxin). It is a specific inhibitor of Ca2+-ATPase.

2,5-Di-t-butylhydroquinone, 99.0+ % (Capillary GC)

040-24681

100 mg

for Biochemistry

88-58-4

Benzene, ethanol,
acetone,

carbon bisulfide

IC50 = 66.7 ± 2.1 μM

Keep at RT.

046-24683

1 g

<Calcium ATPase Inhibitors>

This product inhibits the Ca2+ ATPase of the sarcoplasmic reticulum and does not act on the plasma membrane Ca2+ pump.

E-64d, 97.0+ % (HPLC)

054-08021

1 mg

for Cellbiology

88321-09-9

Methanol

IC50 = 0.5 μM

Keep at -20°C.

050-08023

5 mg

<Calpain inhibitors>

Membrane-permeable cysteine protease inhibitor which is an analog of E-64, a cysteine protease inhibitor isolated from Aspergillus
japonicas. Esters are hydrolyzed when permeated through the membrane and E-64d is considered to change to an activated form, E-64c.
This reagent inhibits calpain and cathepsin. It is used in combination with pepstatin A in order to prevent degradation of LC3-II in the
autophagosome inner membrane during autophagy.

Fluphenazine Dimaleate, 98.0+ % (Titration)

061-01751

1 g

for Biochemistry

3093-66-1

Dilute hydrochloric
acid

-

Keep at 2-10°C.

<Calmodulin antagonists>

Phenothiazine neuroleptic. It is a calmodulin inhibitor, similar to chlorpromazine.

Mastoparan

139-16511

1 mg

for Cellbiology

72093-21-1

Water

IC50 = 15 μM

Keep at -20°C.

<Calmodulin antagonists>

Amphiphilic peptide isolated as an ingredient of hornet poison. It activated directly pertussis toxin-sensitive G protein (Gi, G0) by a
mechanism resembling G protein-conjugate type receptors. It also acts as a calmodulin antagonist.

MG-132, 80.0+ % (HPLC)

139-16251

1 mg

for Cellbiology

133407-82-6

Methanol

IC50 = 1.25 μM

Keep at -20°C.

135-16253

5 mg

<Calpain inhibitors>

Membrane-permeable peptide aldehyde protease inhibitor which reversibly inhibits the chymotrypsin-like activity of 26S proteasome.

Quinacrine Dihydrochloride Dihydrate, 95.0+ % (HPLC)

171-00502

25 g

for Biochemistry

69-05-6

Water, ethanol

IC50 = 4.4 μM

Keep below 25°C.

<Calmodulin antagonists>

Antimalarial; calmodulin inhibitor; phospholipase inhibitor

Suramin Sodium, 98.0+ % (HPLC)

199-10613

100 mg

for Biochemistry

129-46-4

Water

IC50 = 4.9 ± 1.2 μM

Keep at RT.

193-10611

200 mg

<Calcium ATPase Inhibitors>

This product inhibits Ca2+ ATPase of the sarcoplasmic reticulum. It also blocks growth factors, including EGF from binding to the cell
envelope.

Thapsigargin

209-17281

1 mg

for Cellbiology

67526-95-8

Acetonitrile

IC50 = 0.13 ± 0.02 μM

Keep at -20°C.

205-17283

5 mg

<Calcium ATPase Inhibitors>

Thapsigargin is an endoplasmic reticulum Ca2+-ATPase(SERCA) inhibitor which inhibits all SERCA isoforms. The endoplasmic reticulum
uptake of calcium ion is blocked causing releasing of calcium ions from the endoplasmic reticulum to the cytoplasm, by irreversible inhibition
of SERCA activity.

indexpage top

5. Ion Channel-related Blockers

Product Name

Wako Cat. No.

Pkg. Size

Grade/Manufacturer

CAS No.

Soluble in

IC50

Storage Condition

Summary

(1) Calcium Channel Blockers

ω-Agatoxin IVA (P-type Blocker), from Funnel Web Spider, Agelenopsis aperta

339-42561

0.1 mg

Peptide Institute, Inc.

(4256-s)

145017-83-0

-

-

Keep at -20°C.

Channel selective blockers with Cys-Cys binding. Peptidic ion channel blockers.

ω-Agatoxin TK (P-type Blocker)

339-42941

0.1 mg

Peptide Institute, Inc.

(4294-s)

145017-83-0

-

-

Keep at -20°C.

Channel selective blockers with Cys-Cys binding. Peptidic ion channel blockers.

Agelenin, from Spider, Agelena opulenta

330-42471

0.1 mg

Peptide Institute, Inc.

(4247-s)

-

-

-

Keep at -20°C.

Channel selective blockers with Cys-Cys binding. Peptidic ion channel blockers.

Amlodipine, 98.0+ % (HPLC)

011-24951

100 mg

for Cellbiology

88150-42-9

-

-

Keep at RT.

017-24953

1 g

L-type calcium channel blocker with a hypotensive action.

It acts on cardiovascular system, including facilitation of NO production, inhibition of oxidative stress, and inhibition of adhesion of
monocytes to the endothelium. In addition, it acts for a prolonged period compared to other similar calcium channel blockers.

2,3-Butanedione Oxime

045-00652

 25 g

Wako Special Grade

57-71-6

Water, ethanol

IC50 = 15.3 mM

Keep at RT.

047-00651

100 g

2,3-Butanedione Oxime has phosphatase activity and inhibits contraction of skeletal muscles and cardiac muscles.

Calcicludine (L-type Blocker), 99.0+ % (HPLC), from Green Mamba, Dendroaspis angusticeps

337-43101

0.1 mg

Peptide Institute, Inc.

(4310-s)

178037-96-2

-

-

Keep at -20°C.

Neuronal L-type Ca2+ Channel Blocker. Peptidic ion channel blockers.

Calciseptine (L-type Blocker), from Black mamba, Dendroaspis polylepis polylepis

332-42551

0.1 mg

Peptide Institute, Inc.

(4255-s)

-

-

-

Keep at -20°C.

L-type Ca2+ Channel Blocker. Peptidic ion channel blockers.

Cinnarizine, 98.0+ % (Titration)

030-13592

25 g

for Biochemistry

298-57-7

Acetone, ether,
chloroform,
benzene

IC50 = 0.75 μM

Keep at RT.

Cinnarizine has antihistaminic and vasodilatory activities, improves cerebral blood flow impairment, and exerts Ca2+ channel inhibitory activity.

ω-Conotoxin GVIA (N-type Blocker), from Marine Snail, Conus geographus

336-41611

0.5 mg

Peptide Institute, Inc.

(4161-v)

106375-28-4

-

-

Keep at -20°C.

N-type Ca2+ Channel Blocker. Peptidic ion channel blockers.

ω-Conotoxin MVIIA (N-type Blocker), 99.0+ % (HPLC) from Marine snail, Conus magus

338-42891

0.5 mg

Peptide Institute, Inc.

(4289-v)

107452-89-1

-

-

Keep at -20°C.

Reversible N-type Ca2+ Channel Blocker. Peptidic ion channel blockers.

ω-Conotoxin MVIIC (P/Q-type Blocker), 99.0+ % (HPLC), from Marine Snail, Conus magus

332-42833

0.5 mg

Peptide Institute, Inc.

(4283-v)

147794-23-8

-

-

Keep at -20°C.

336-42831

0.1 mg

Peptide Institute, Inc.

(4283-s)

P/Q-type Ca2+ Channel Blocker. Peptidic ion channel blockers.

ω-Conotoxin SVIB (N-type Blocker), 99.0+ % (HPLC), from Marine Snail, Conus striatus

333-42841

0.5 mg

Peptide Institute, Inc.

(4284-v)

150433-82-2

-

-

Keep at -20°C.

N-type Ca2+ Channel Blocker. Peptidic ion channel blockers.

Diltiazem Hydrochloride, 98.0+ % (Titration)

047-20311

1 g

for Biochemistry

33286-22-5

Formic acid, water,
ethanol, chloroform

IC50 = 4.5 μM

Keep at 2-10°C.

043-20313

5 g

Therapeutic substance for circulatory diseases such as hypertension, angina and arrhythmia.

It inhibits voltage-dependent calcium channels and reduces the inflow of Ca2+ from extracellular to intracellular parts. Specific calcium
antagonists include nifedipine, verapamil and diltiazem.

Kurtoxin, 98.0+ % (HPLC), from Scorpion, Parabuthus transvaalicus

338-43751

0.1 mg

Peptide Institute, Inc.

(4375-s)

-

-

-

Keep at -20°C.

T-type Ca2+ channel blocker. Peptidic ion channel blockers.

Nicardipine Hydrochloride, 99.0+ % (HPLC)

145-06381

1 g

for Biochemistry

54527-84-3

Methanol,
chloroform

IC50 = 2.56 μM

Keep at RT.

141-06383

5 g

It inhibits voltage-dependent calcium channels and reduces the inflow of Ca2+ from extracellular to intracellular parts.

Nitrendipine, 98.0+ % (HPLC)

142-06411

200 mg

for Biochemistry

39562-70-4

Chloroform,
acetonitrile

IC50 = 23 μM

Keep at RT.

It inhibits voltage-dependent calcium channels and reduces the inflow of Ca2+ from extracellular to intracellular parts. It dilates peripheral
vessels and coronary arteries and has hypotensive and anti-angina actions. Its hypotensive action is comparable to nifedipine, and the action
lasts longer than nifedipine.

PLTX-II, 99.0+ % (HPLC), from Spide, Plectreurys tristes

331-43001

0.1 mg

Peptide Institute, Inc.

(4300-s)

-

-

-

Keep at -20°C.

Presynaptic Ca2+ Channel Blocker

ProTx-1, 97.0+ % (HPLC), from Tarantula, Thrixopelma pruriens

338-44091

0.1 mg

Peptide Institute, Inc.

(4409-s)

-

-

-

Keep at -20°C.

T-Type Ca2+ Channel / Na+ Channel / K+ Channel Blocker (Gating Modifier)

Ryanodine

185-02821

1 mg

for Cellbiology

15662-33-6

Methanol

-

Keep at -20°C.

Signal transduction Ca2+ channel Inhibitor Ryanodine is an alkaloid isolated from Ryania speciosa Vahl. It acts to increase calcium
permeability by binding to the arcoplasmic reticulum calcium channel.

SNX-482, 99.0+ % (HPLC), from Tarantula, Hysterocrates gigas

338-43631

0.1 mg

Peptide Institute, Inc.

(4363-s)

203460-30-4

-

-

Keep at -20°C.

Class E (R-type) Ca2+ Channel Blocker

Verapamil Hydrochloride, 98.0+ % (Titration)

222-00781

 1 g

for Biochemistry

152-11-4

Ethanol

IC50 = 0.3 μM

Keep at RT.

228-00783

10 g

Verapamil HCl directly affects the smooth muscle of blood vessels and the heart and is a Ca2+ antagonist. It also promotes effects of
tumoricidal drugs and is used in research concerning the mechanism of calcium antagonists.

(2) Potassium Channel Blockers

Apamin, 99.0+ % (HPLC), from Honeybee, Apis mellifera

336-42571

0.5 mg

Peptide Institute, Inc.

(4257-v)

24345-16-2

-

-

Keep at -20°C.

Small conductance Ca2+-activated K+ channel blocker

Charybdotoxin, 99.0+ % (HPLC), from Scorpion, Leiurus quinquestriatus var. hebraeus

338-42271

0.1 mg

Peptide Institute, Inc.

(4227-s)

95751-30-7

-

-

Keep at -20°C.

Ca2+-activated K+ channel blocker

Dendrotoxin 1, 99.0+ % (HPLC), from black mamba, Dednroaspis polylepis polylepis

339-43301

0.1 mg

Peptide Institute, Inc.

(4330-s)

107950-33-4

-

-

Keep at -20°C.

Voltage-dependent K+ channel blocker

E-4031 n-Hydrate, 98.0+ % (HPLC)

059-08451

10 mg

for Cellbiology

-

Water

Native guinea pig HERG channel: IC50 =
397 nM

Keep at -20°C.

055-08453

50 mg

E-4031 is a HERG potassium channel blocker with antiarrhythmic action (class III ). It selectively inhibits Ikr, a rapid component of the delayed
rectifier K current, during repolarization after muscle cells are depolarized.

Glibenclamide, 98.0+ % (Titration)

078-03881

 5 g

for Biochemistry

10238-21-8

DMF

IC50 = 0.1 μM

Keep at RT.

076-03882

25 g

<Potassium Channel Blockers>

Sulfonylurea hypoglycemic substance. It blocks ATP-dependent K+ channel of the pancreas to increase intracellular Ca2+, thus increasing
insulin secretion. It pharmacologically antagonizes the action of K+ channel-opening agents in the heart and blood vessels.

Guangxitoxin-1E, 97.0+ % (HPLC), from Tarantula, Plesiophrictus guangxiensis sp. nov.

334-44331

0.1 mg

Peptide Institute, Inc.

(4433-s)

-

-

-

Keep at -20°C.

Kv2.1/Kv2.2 channel blocker / Enhancer of glucose-dependent insulin secretion

Iberiotoxin, 99.0+ % (HPLC), from Scorpion, Buthus tamulus

330-42351

0.1 mg

Peptide Institute, Inc.

(4235-s)

129203-60-7

-

-

Keep at -20°C.

Highly selective and potent high conductance Ca2+-activated K+ channel blocker

Kaliotoxin (1-37), 99.0+ % (HPLC), from Scorpion, Androctonus mauretanicus mauretanicus

330-42591

0.1 mg

Peptide Institute, Inc.

(4259-s)

145199-73-1

-

-

Keep at -20°C.

High conductance Ca2+-activated K+ channel blocker

Margatoxin 【MgTX】, 99.0+ % (HPLC)

331-42901

0.1 mg

Peptide Institute, Inc.

(4290-s)

145808-47-5

-

-

Keep at -20°C.

Voltage-dependent K+ channel blocker (specific for Kv1.3 channel )

MCD-Peptide, 99.0+ % (HPLC), from Honeybee, Apis mellifera

333-42581

0.5 mg

Peptide Institute, Inc.

(4258-v)

32908-73-9

-

-

Keep at -20°C.

Voltage-dependent K+ channel blocker

Scyllatoxin, 99.0+ % (HPLC), from Scorpion, Leiurus quinquestriatus hebraeus

333-42601

0.1 mg

Peptide Institute, Inc.

(4260-s)

116235-63-3

-

-

Keep at -20°C.

Small conductance Ca2+-activated K+ channel blocker

Stichodactyla Toxin, 99.0+ % (HPLC), from Sea Anemone, Stichodactyla helianthus

334-42871

0.1 mg

Peptide Institute, Inc.

(4287-s)

-

-

-

Keep at -20°C.

Voltage-dependent K+ channel (A channel) blocker

Tertiapin, 99.0+ % (HPLC), from Apis mellifera

335-43641

0.1 mg

Peptide Institute, Inc.

(4364-s)

58694-52-3

-

-

Keep at -20°C.

Potent blocker of inward-rectifier K+ channels such as ROMK1 and GIRK1/4 at 2.5-10 nM.

Tityustoxin Kα, 99.0+ % (HPLC), from Scorpion, Tityus serrulatus

338-43131

0.1 mg

Peptide Institute, Inc.

(4313-s)

39465-37-7

-

-

Keep at -20°C.

Voltage-dependent K+ channel (A channel) blocker

(3) Sodium Channel Blockers

Clotrimazole, 98.0+ % (HPLC)

035-16021

5 g

for Biochemistry

23593-75-1

Ethanol, chloroform,
carbon tetrachloride

IC50 = 1.8 μM

Keep at RT.

033-16022

25 g

It exhibits bactericidal action by destroying cytoplasmic membranes of fungi.

μ-Conotoxin G3B, 99.0+ % (HPLC), from Marine Snail, Conus geographus

332-42171

0.5 mg

Peptide Institute, Inc.

(4217-v)

140678-12-2

-

-

Keep at -20°C.

Na+ channel blocker: Specific for skeletal muscle

μ-Conotoxin GS, 95.0+ % (HPLC), from Marine Snail, Conus geographus

334-42631

0.5 mg

Peptide Institute, Inc.

(4263-v)

171358-00-2

-

-

Keep at -20°C.

Selective blocker of Na+ channels of skeletal muscles.

μ-Conotoxin SIIIA, 99.0+ % (HPLC), from Marine Snail, Conus striatus

339-44401

0.5 mg

Peptide Institute, Inc.

(4440-v)

877860-32-7

-

-

Keep at -20°C.

Tetrodotoxin-resistant Na+ channel blocker with analgesic activity

Huwentoxin-IV, 97.0+ % (HPLC), from Chinese Bird Spider, Ornithoctonus huwena

330-44551

0.1 mg

Peptide Institute, Inc.

(4455-s)

-

-

-

Keep at -20°C.

Neuronal tetrodotoxin-sensitive Na+-channel blocker

Omeprazole, 98.0+ % (HPLC)

150-02091

10 g

for Biochemistry

73590-58-6

Dichloromethane,
methanol

IC50 = 4.2 μM

Keep at -20°C.

158-02092

25 g

Eradicating agent for Helicobacter pylori (HP).

Selective inhibitor of gastric H+, K+ ATPase (proton pump), and used as a marker to test the susceptibility of HP to this product in vitro.

ProTx-II, 99.0+ % (HPLC)

335-44501

0.1 mg

Peptide Institute, Inc.

4450-s

-

-

-

Keep at -20°C.

Na+ channel (especially Nav1.7) / Ca2+ channel blocker (gating modifier)

(4) Transient Receptor Potential (TRP) Channel Blockers

AMG 9810, 98.0+ % (HPLC)

015-25071

10 mg

for Cellbiology

545395-94-6

Ethanol

-

Keep at 2-10°C.

011-25073

50 mg

Antagonist of transient receptor potential vanilloid 1 (TRPV1). TRPV1 is one of the TRP channels cloned as a capsaicin receptor, functions
as a pain receptor, and is activated by capsaicin, heat, and protons. It also inhibits the activation of TRPV1 by heat and protons, besides
capsaicin.

AP 18, 98.0+ % (HPLC)

014-25161

10 mg

for Cellbiology

55224-94-7

Ethanol

(10 mg/2 mL)

-

Keep at -20°C.

010-25163

50 mg

Selective TRPA1 (transient receptor potential ankyrin 1) inhibitor. TRPA1 is involved in pain transmission, and its involvement in respiratory
depression has also been reported.

2-APB, 98.0+ % (HPLC)

013-24911

100 mg

for Cellbiology

524-95-8

Ethanol

-

Keep at -20°C.

019-24913

500 mg

Inhibitor of inositol triphosphate (IP3) receptors. It can also block TRP channels TRPC1, TRPC3, TRPC5, TRPC6, TRPV6, TRPM3, TRPM7,
TRPM8 and TRPP2. At high concentrations, it can activate TRPV1, TRPV2 and TRPV3.

BCTC, 98.0+ % (HPLC)

027-18241

10 mg

for Cellbiology

393514-24-4

Ethanol

-

Keep at -20°C.

023-18243

50 mg

TRPV1 antagonist. It inhibits the activation of TRPV1 by capsaicin and acids.

Capsazepine, 98.0+ % (HPLC)

037-23171

10 mg

for Cellbiology

138977-28-3

Ethanol

-

Keep at 2-10°C.

033-23173

50 mg

TRPV1 antagonist. Capsaicin analog.

HC-030031, 98.0+ % (HPLC)

086-09961

10 mg

for Cellbiology

349085-38-7

DMSO

-

Keep at RT.

082-09963

50 mg

Selective TRPA1 (transient receptor potential ankyrin 1) inhibitor.

Olvanil, 98.0+ % (HPLC)

154-03231

10 mg

for Cellbiology

58493-49-5

Ethanol

-

Keep at -20°C.

150-03233

50 mg

It demonstrated to block intracellular accumulation of Anandamide through interaction with the anandamide transporter at concentrations
similar to those needed for TRPV1 activation. Also inhibits FAAH (fatty acid amide hydrolase). It also acts as a potent TRPV1 angonist and a
CB1 agonist.

RN-1747, 98.0+ % (HPLC)

183-02981

10 mg

for Cellbiology

1024448-59-6

DMSO

-

Keep at 2-10°C.

189-02983

50 mg

TRPM8 antagonist. It also acts as a TRPV4 (transient receptor potential vanilloid 4)-selective agonist.

Ruthenium Red

184-00331

100 mg

Wako Special Grade

11103-72-3

Water

-

Keep at RT.

180-00333

1 g

TRPA1 antagonist.

SB-366791, 98.0+ % (HPLC)

193-17431

10 mg

for Cellbiology

472981-92-3

Ethanol

-

Keep at -20°C.

199-17433

50 mg

TRPV1 antagonist, which inhibits the activation of TRPV1 by capsaicin and heat. It has been reported that it does not inhibit activation by
protons.

(5) Acid-Sensing Ion Channel Blockers

APETx2, 99.0+ % (HPLC)

331-44721

0.1 mg

Peptide Institute, Inc.

(4472-s)

713544-47-9

-

-

Keep at -20°C.

Selective blocker of acid-sensing ion channel blocker, ASIC3

Psalmotoxin 1, 97.0+ % (HPLC), from South American Tarantula, Psalmopoeus cambridgei (Trifluoroacetate Form)

338-44351

0.1 mg

Peptide Institute, Inc.

(4435-s)

-

-

-

Keep at -20°C.

Selective blocker of ASIC1a

(6) Nicotinic Acetylcholine Receptor Blockers

α-Conotoxin G1, 97.0+ % (HPLC), from Marine Snail, Conus geographus (Hydrochloride Form)

337-41261

0.5 mg

Peptide Institute, Inc.

(4126-v)

76862-65-2

-

-

Keep at -20°C.

Nicotinic acetylcholine receptor blocker

α-Conotoxin ImI, 99.0+ % (HPLC), from Marine Snail, Conus imperialis

334-43111

0.5 mg

Peptide Institute, Inc.

(4311-v)

156467-85-5

-

-

Keep at -20°C.

Nicotinic acetylcholine receptor blocker in central nervous system

α-Conotoxin M1, 99.0+ % (HPLC), from Marine Snail, Conus magus

337-41401

0.5 mg

Peptide Institute, Inc.

(4140-v)

88217-10-1

-

-

Keep at -20°C.

Nicotinic acetylcholine receptor blocker

α-Conotoxin SI, 99.0+ % (HPLC), from Marine Snail, Conus striatus

335-42281

0.5 mg

Peptide Institute, Inc.

(4228-v)

133605-58-0

-

-

Keep at -20°C.

Nicotinic acetylcholine receptor blocker

(7) Other Blockers

Chlorotoxin, 99.0+ % (HPLC), from Scorpion, Leiurus quinquestriatus

339-42821

0.5 mg

Peptide Institute, Inc.

(4282-v)

163515-35-3

-

-

Keep at -20°C.

Small-conductance Cl- channel blocker

GsMTx-4, 99.0+ % (HPLC)

336-43931

0.1 mg

Peptide Institute, Inc.

(4393-s)

-

-

-

Keep at -20°C.

Inhibitor for cation-selective stretch-activated channels / Atrial fibrillation inhibiting peptide

Purotoxin-1, 99.0+ % (HPLC)

334-44571

0.1 mg

Peptide Institute, Inc.

(4457-s)

-

-

-

Keep at -20°C.

P2X3 purinoreceptor inhibitor

indexpage top

6.G-protein Signaling and Second Messenger-related Inhibitors

Product Name

Wako Cat. No.

Pkg. Size

Grade/Manufacturer

CAS No.

Soluble in

IC50

Storage Condition

Summary

Andrographolide, 98.0+ % (HPLC)

014-15271

500 mg

for Biochemistry

5508-58-7

Methanol, acetone

IC50 = 5.6 ± 0.7 μM

Keep at 2-10°C.

<Guanylate Cyclase Inhibitors>

It is reported to suppress the decrease of glutathion and to counteract toxic liver damage caused by substances such as carbontetrachloride
and t-butylhydroperoxide.

BAY 11-7085, 98+ % (NMR)

020-14331

10 mg

for Biochemistry

196309-76-9

Ethanol, acetone

IC50 = 10 μM

Keep at -20°C.

026-14333

25 mg

<NFκB Inhibitors>

Inhibitor of cytokine-induced IκBα phosphorylation and decreases expression of NFκB and adhesion molecule. It also exhibits strong
antiinflammatory activity.

8-(4-Chlorophenylthio)adenosine 3',5'-(Cyclic)monophosphate Sodium Salt, 98.0+ % (HPLC)

039-18121

 10 mg

for Biochemistry

93882-12-3

Water

IC50 of PKA: 900 nM; PKG: 25 μM

Keep at -20°C.

035-18123

100 mg

<Adenylate Cyclase Inhibitors>

Cell permeable cAMP analog, used as an activator of cAMP-dependent protein kinase (PKA) and cGMP-dependent protein kinase (PKG).

Curcumin

038-04921

 1 g

Wako Special Grade

458-37-7

Ethanol, acetic acid

IC50 of 5-Lipoxygenase: 5 - 10 μM,
COX ≦ 100 μM

Keep at RT.

036-04922

25 g

<Guanylate Cyclase Inhibitors>

Inhibitor of 5-lipoxygenase and cyclooxygenase.

Isotetrandrine

306-01771

25 mg

Kaken Shoyaku Co.,
Ltd.

477-57-6

-

-

Keep at 2-10°C.

<G-protein Signaling Inhibitor>

A biscoclaurine alkaloid inhibitor of G protein activation of PLA2

LY-83583, 94+ % (TLC)

128-04691

5 mg

for Biochemistry

91300-60-6

Ethanol, acetone

IC50 of soluble Guanylate cyclase in human
platelets: 2 μM; leukotriene synthesis in
guinea pig lung and rat celiac cells: 1.8 μM

Keep at -20°C.

<Guanylate Cyclase Inhibitors>

It decreases the concentration of cellular cGMP through the inhibition of guanylate cyclase.

NS2028, 98.0+ % (HPLC)

149-06921

5 mg

for Biochemistry

204326-43-2

Water, ethanol

-

Keep at -20°C.

<Guanylate Cyclase Inhibitors>

Selective inhibitor of soluble guanylate cyclase (sGC) that is sensitive to NO. It does not inhibit sGC activity enhanced by YC-1 or CO.

1H-[1,2,4]Oxadiazolo[4,3-a]quinoxalin-1-one 【ODQ】, 97.0+ % (HPLC)

153-01981

10 mg

for Biochemistry

41443-28-1

Ethanol, acetone

-

Keep at 2-10°C.

159-01983

25 mg

<Guanylate Cyclase Inhibitors>

It inhibits the guanylate cyclase activity of NO produced by NOS rather than NO synthase (NOS), and controls the increase in cGMP.

Pentoxifylline, 98.0+ % (Titration)

160-18761

10 g

for Biochemistry

6493-05-6

Methanol, ethanol,
acetone, water

TNFα: IC50 = 100 μM

Keep at RT.

<Guanylate Cyclase Inhibitors>

TNF-α synthesis inhibior and phosphodiesterase inhibitor

Rolipram, 98+ % (TLC)

180-01411

10 mg

for Biochemistry

61413-54-5

Ethanol

IC50 = 20 μM

Keep at 2-10°C.

<NFκB Inhibitors>

This cAMP diphosphodiesterase inhibitor selectively inhibits phosphodiesterase IV, a type of isozyme. Improvement of arthritis (in rats with
collagen II induced arthritis) has been reported.

indexpage top

7.Neurotransmitter Inhibitors

Product Name

Wako Cat. No.

Pkg. Size

Grade/Manufacturer

CAS No.

Soluble in

IC50

Storage Condition

Summary

(1) Glutamate Receptor Antagonists

DL-2-Amino-4-phosphonobutyric Acid, 98.0+ % (HPLC)

013-22071

100 mg

for Cellbiology

6323-99-5

Hydrochloric acid,
water

-

Keep at 2-10°C.

NMDA-type glutamate receptor antagonists.

L-2-Amino-4-phosphonobutyric Acid, 98.0+ % (HPLC)

016-22083

10 mg

for Cellbiology

23052-81-5

Water

EC50 = 16.0 μM

Keep at 2-10°C.

Selective agonist for group III metabotropic glutamate receptors ( mgluR4, mgluR6).

D(-)-2-Amino-5-phosphonovaleric Acid 【D-AP5】

015-18481

10 mg

for Biochemistry

79055-68-8

Hydrochloric acid

IC50 = 3.7 ± 0.32 μM

Keep at RT.

A neural amino acid. It is a potent antagonist of the NMDA-type receptor, which is one of the ion-channel glutamine receptors.

DL-2-Amino-5-phosphonovaleric Acid 【DL-AP5】

018-18471

10 mg

for Biochemistry

76326-31-3

Water

IC50 = 90 μM

Keep at RT.

A neural amino acid. It is a potent antagonist of the NMDA-type receptor, which is one of the ion-channel glutamine receptors.

(R)-CPP

031-22091

1 mg

for Cellbiology

126453-07-4

Water (10 mg/mL)

-

Keep at RT.

037-22093

5 mg

Highly potent glutaminergic NMDA receptor antagonist. It exhibits a higher activity than racemic CPP. It is selective to NR2A in NMDA
receptor.

Dextromethorphan Hydrobromide Monohydrate, 98.0+ % (Titration)

041-21551

 5 g

for Biochemistry

6700-34-1

Methanol, acetic
acid, ethanol

-

Keep below 25°C.

049-21552

25 g

NMDA receptor antagonist.

Diazoxide, 99.0+ % (HPLC)

047-23133

250 mg

for Biochemistry

364-98-7

DMSO

-

Keep at RT.

041-23131

1 g

Desensitization blocker of AMPA receptor.

DL-AP7, 98.0+ % (1H- NMR)

041-31941

5 mg

for Cellbiology

85797-13-3

NaOH soln.

IC50 = 11.1 ± 2.1 μM

Keep at RT.

A neural amino acid. It is a potent antagonist of the NMDA-type receptor, which is one of the ion-channel glutamine receptors.

DNQX, 95+ % (TLC)

044-26301

50 mg

for Biochemistry

2379-57-9

Methanol

-

Keep at -20°C.

AMPA/Kainate receptor antagonist

Evans Blue

056-04061

 5 g

Practical Grade

314-13-6

Water

IC50 = 87 nM

Keep at RT.

054-04062

25 g

AMPA/Kainate receptor antagonist.

Felbamate, 98.0+ % (HPLC)

060-05861

10 mg

for Cellbiology

25451-15-4

DMSO, ethanol

IC50 = 0.78 ± 0.07 mM

Keep at -20°C.

066-05863

50 mg

Allosteric antagonist of NR2B subunit of glutaminergic NMDA receptor and exhibits strong anticonvulsant action. It also has a property as a
γ-aminobutyric acid (GABA) receptor agonist.

Joro Spider Toxin JSTX-3, 98.0+ % (HPLC)

104-00051

0.1 mg

for Biochemistry

112163-33-4

Water

IC50 = 1.7 μM

Keep at 2-10°C.

Toxin isolated from Joro Spider poison gland, paralyzes the movement of arthropods (insects, crustaceans, etc.). It irreversibly blocks
excitatory transmissions of neurons and muscles by glutamate released from the synaptic terminal of motor neurons. It acts selectively on
quisqualate glutamate receptor.

Loperamide Hydrochloride

129-05721

 5 g

for Pharmacology
Research

34552-83-5

Methanol, ethanol

IC50 = 0.9 ± 0.2 μM

Keep at RT.

127-05722

25 g

NMDA receptor antagonist. It reduces Ca2+ flow. Loperamide Hydrochloride is a NMDA receptor antagonist that reduces the flow of Ca2+.
It is an antidiarrheal agent that inhibits both peristaltic movement of the intestinal tract and secretion, and enhances absorption, via opioid
receptor in the intestinal tract.

(+)-MCPG, 99.0+ % (HPLC)

135-16111

 2 mg

for Cellbiology

150145-89-4

0.1M NaOH

IC50 = 272 μM

Keep at 2-10°C.

131-16113

10 mg

Competitive antagonist for group 1 (mGluR1, mGluR5) and group 2 (mGluR2, mGluR3) metabotropic glutamate receptors. It is an active
enantiomer of (±)-MCPG.

Memantine Hydrochloride

132-16981

 25 mg

for Cellbiology

41100-52-1

Water

IC50 = 1.2 ± 0.2 μM

Keep at RT.

138-16983

100 mg

This is a glutaminergic NMDA receptor antagonist and stimulates dopamine release by binding to the ion channel site. It is used in
researches on Parkinson's disease, spasms, Alzheimer's disease and so on.

(+)-MK 801 Maleate, 98.0+ % (HPLC)

130-17381

10 mg

for Cellbiology

77086-22-7

Methanol

Ki = 30.5 ± 1.5 nM

Keep at 2-10°C.

136-17383

50 mg

Selective antagonist of NMDA glutamate receptor. It inhibits calcium ion influx across cell membranes by binding mainly to the pore of the
ion channel opened upon the ligand binding. It is known as an anti-ischemic agent.

NBQX Disodium Salt, 98.0+ % (HPLC)

147-08661

10 mg

for Cellbiology

479347-86-9

Water

-

Keep at 2-10°C.

Water-soluble NBQX. NBQX is a potent and competitive AMPA/kainate receptor antagonist.

NBQX, 99+ % (TLC)

148-06751

10 mg

for Biochemistry

118876-58-7

Acetone

IC50 = 0.90 μM

Keep at 2-10°C.

Antagonist of the AMPA/kainate receptor.

Pentamidine Isethionate, 98.0+ % (HPLC)

166-25191

50 mg

for Cellbiology

140-64-7

Water

IC50 = 2 - 18 μM

Keep at -20°C.

This substance exhibits nerve protection activity and inhibits homeostatic NO synthase in the brain. It is an antagonist to NMDA glutamate
receptor. It inhibits glucose metabolism and protein synthesis in Pneumocystis carinii.

Spermine, 95.0+ % (Titration)

198-09811

250 mg

for Biochemistry

71-44-3

Water, chloroform

IC50 = 170 μM

Keep at 2-10°C.

194-09813

1 g

Agonist during depolarization and antagonist during hyperpolarization.

(2) Inhibitors of Angiotensin Conversion Enzyme

Benazepril Hydrochloride, 97.0+ % (HPLC)

024-14091

1 g

for Biochemistry

86541-74-4

Ethanol

-

Keep at RT.

020-14093

5 g

ACE inhibitor used clinically as a therapeutic for hypertension.

Captopril, 96.0+ % (Titration)

039-20951

 1 g

for Pharmacology
Research

62571-86-2

Methanol, acetone,
water

IC50 = 9 nM

Keep below 25°C.

035-20953

 5 g

037-20952

25 g

Angiotensin converting enzyme (ACE) inhibitor that blocks ACE and inhibits the pressor system while enhancing the depressor system. It is a
crude drug for essential and renal hypertensions.

Enalaprilat Dihydrate, 98.0+ % (HPLC)

055-06851

1 g

for Biochemistry

84680-54-6

Methanol

IC50 = 4.8 nM

Keep at RT.

This is an active form of enalapril, which is an angiotensin converting enzyme (ACE) inhibitor. One of the percutaneous vasodilators.

Enalapril Maleate, 98.0+ % (HPLC)

051-06711

1 g

for Biochemistry

76095-16-4

Methanol, ethanol

IC50 = 1 - 10 nM

Keep at RT.

057-06713

5 g

It inhibits angiotensin II synthesis by inhibiting angiotensin converting enzyme.

Lisinopril Dihydrate, 98.0+ % (HPLC)

128-04711

1 g

for Biochemistry

76547-98-3

Water

IC50 = 1.2 nM

Keep at RT.

124-04713

5 g

It inhibits angiotensin II production by blocking angiotensin converting enzyme, and has antihypertensive effects. It is a crude drug for
treating hypertension, chronic heart failure, etc.

(3) Cannabinoid Receptor Antagonists

AACOCF3

011-18461

10 mg

for Biochemistry

149301-79-1

Ethanol

IC50 = 15 μM

Keep at -20°C.

Selective inhibitor of cellular phospholipase A2 (cPLA2) and Ca2+ independent phospholipase A2 (iPLA2) (IC50 = 15 μM).

AM 251, 95.0+ % (HPLC)

011-24191

 2 mg

for Cellbiology

183232-66-8

DMSO, DMF

IC50 = 8.9 μM

Keep at -20°C.

017-24193

10 mg

015-24194

50 mg

Potent CB1 receptor antagonist/inverse agonist. Ki = 7.5 nM. It is an analog of a cannabinoid receptor antagonist, SR141716A.

AM 281, 97.0+ % (HPLC)

012-22161

 2 mg

for Cellbiology

202463-68-1

Methanol

IC50 = 6 nM

Keep at 2-10°C.

018-22163

10 mg

Potent CB1 receptor antagonist/inverse agonist. Ki = 14 nM. It is an analog of a cannabinoid receptor antagonist, SR141716A.

AM 630

019-22551

 2 mg

for Cellbiology

164178-33-0

DMSO

IC50 = 6.3 μM

Keep at 2-10°C.

015-22553

10 mg

Antagonist/inverse agonist of cannabinoid receptor subtype CB2 (Ki = 31.2 nM).

(4) GABA Receptor Antagonists

(+)-Bicuculline, 98.0+ % (HPLC)

026-16131

 50 mg

for Cellbiology

485-49-4

Methanol,
chloroform

IC50 = 4.5 μM

Keep at -20°C.

022-16133

250 mg

Lactone of bixin, known for its use as a proconvulsant. It is a selective antagonist of GABA(A) receptor, a GABA receptor subtype that exists
in the central and peripheral nervous systems. Because this reagent binds to GABA binding site, it competitively blocks GABA and muscimol
actions.

(-)-Bicuculline Methobromide

026-14291

100 mg

for Biochemistry

73604-30-5

Water

IC50 = 15 nM

Keep at 2-10°C.

GABAA receptor antagonist.

(-)-Bicuculline Methochloride, 93.0+ % (HPLC)

026-17611

10 mg

for Biochemistry

53552-05-9

-

IC50 = 0.8 ± 0.2 μM

Keep at -20°C.

022-17613

50 mg

Water-soluble methochloride salt of (+)-bicuculline

Picrotoxin, 97.0+ % (HPLC)

168-17961

1 g

Wako 1st Grade

124-87-8

Ethanol

IC50 = 2.6 ± 0.4 μM

Keep at RT.

164-17963

5 g

GABAA receptor antagonist.

Picrotoxinin, 95.0+ % (HPLC)

165-17351

500 mg

for Biochemistry

17617-45-7

Ethanol, Chloroform

IC50 = 25 ± 0.4 μM

Keep at 2-10°C.

A bitter component isolated from a plant of family Menispermaceae (Anamirta cocculus). The toxic moiety of picrotoxin (central nerve
excitation agent), which blocks the Cl- channel in an allosterical manner that forms a molecular complex with GABA receptors.

(5) Serotonin-related Inhibitors

Amitriptyline Hydrochloride, 99.0+ % (Titration)

013-12882

25 g

for Biochemistry

549-18-8

Water, chloroform,
ethanol

5-HT: IC50 = 39 nM

NA: IC50 = 21 nM

Keep at RT.

Tricyclic antidepressant substance, anxiolytic substance. It inhibits reuptake of noradrenaline and serotonin in the brain and exerts an
antidepressant action.

Amoxapine, 98.0+ % (HPLC)

015-23631

1 g

for Pharmacology
Research

14028-44-5

Acetic acid,

glacial, chloroform,
dichloroethane

-

Keep at RT.

011-23633

5 g

This is a tricyclic antidepressant. It inhibits reuptake of serotonin (5-HT) and noradrenaline in nerve terminals in the brain.

Azasetron Hydrochloride, 90.0+ % (HPLC)

014-24441

 50 mg

for Biochemistry

123040-16-4

Water

-

 

010-24443

200 mg

5-HT3 Receptor Antagonist

Blonanserin, 98.0+ % (HPLC)

022-17451

 5 mg

for Pharmacology
Research

132810-10-7

Acetonitrile, acetic
acid, methanol,
ethanol

Ki = 0.812 nM (5-HT2A); 0.142 nM
(Dopamine D2); 0.494 nM (Dopamine D3)

Keep at RT.

028-17453

50 mg

This substance binds selectively to dopamine D2 receptor and serotonin 5-HT2 receptor and exhibits antagonistic activities.

DL-p-Chlorophenylalanine, 99.0+ % (Titration)

037-10741

 1 g

Wako Special Grade

7424-00-2

Dilute hydrochloric
acid

-

Keep at RT.

033-10743

 5 g

035-10742

25 g

It irreversibly binds to tryptophan hydroxylase and decreases intracerebral serotonin (serotonin synthetic inhibitor).

Citalopram Hydrobromide, 98.0+ % (HPLC)

031-22231

 25 mg

for Pharmacology
Research

59729-32-7

Water, ethanol

IC50 = 1.8 nM

Keep at 2-10°C.

037-22233

100 mg

Citalopram Hydrobromide is a selective serotonin reuptake inhibitor (SSRI). This reagent blocks the reuptake of intracerebral serotonin
and exhibits antidepressive effects by increasing serotonin in the synaptic cleft. It is considered to have almost no affinity for other
neurotransmitter receptors.

Clomipramine Hydrochloride, 98.0+ % (volumetric analysis), 98.0+ % (HPLC)

036-21941

1 g

for Pharmacology
Research

17321-77-6

Water, acetic
acid, methanol,
chloroform

IC50 of 5-HT: 1.5 nM; NA: 24 nM

Keep at RT.

032-21943

5 g

Clomipramine Hydrochloride is a derivative of imipramine and has tricyclic antidepressant effects. This reagent blocks the uptake of
intracerebral serotonin (5-HT) and noradrenaline into the nerve terminal. It potently blocks serotonin uptake.

Desipramine Hydrochloride, 99.0+ % (Titration); 99+ % (TLC)

044-23121

1 g

for Biochemistry

58-28-6

Chloroform, water,
ethanol

IC50 of 5-HT: 382 nM; NA: 1.26 nM

Keep at RT.

040-23123

5 g

Tricyclic antidepressant. It binds to amine transporter and blocks reuptake of intracerebral serotonin (5-HT) and noradrenaline into the nerve
terminal. It is an active metabolite of imipramine.

Doxepin Hydrochloride (mixture of isomers), 98.0+ % (HPLC)

043-32001

1 g

for Pharmacology
Research

1229-29-4

Water

IC50 of 5-HT: 280 nM; NA: 40 nM

Keep at RT.

049-32003

5 g

Tricyclic antidepressant. It blocks the reuptake of serotonin and noradrenaline. It is a potent H1 histamine receptor antagonist.

Duloxetine Hydrochloride, 98.0+ % (HPLC)

041-32041

 10 mg

for Pharmacology
Research

136434-34-9

Methanol, DMSO

IC50 of 5-HT: 6.3 nM; NA: 5.8 nM

Keep at RT.

047-32043

100 mg

Tricyclic antidepressant. It blocks the reuptake of serotonin and noradrenaline. It is a potent H1 histamine receptor antagonist.

(±)-Fluoxetine Hydrochloride, 98.0+ % (HPLC)

068-04321

10 mg

for Biochemistry

56296-78-7

Methanol, ethanol,
acetonitrile,
chloroform,

acetone

IC50 = 6.8 nM

Keep below 25°C.

064-04323

50 mg

068-04326

1 g

Selective serotonin reuptake inhibitor (SSRI). It inhibits serotonin reuptake and consequently elevates serotonin concentration in synaptic
gaps exhibiting antidepressive effect.

Fluvoxamine Maleate

065-05171

  5 g

for Pharmacology
Research

61718-82-9

Ethanol

IC50 = 0.29 nM

Keep at 2-10°C.

061-05173

100 g

Selective serotonin reuptake inhibitor (SSRI). It is used for treating melancholia, depression, obsessive compulsive disorder, and social
anxiety disorder.

Granisetron Hydrochloride, 98.0+ % (HPLC)

073-06131

 5 mg

for Pharmacology
Research

107007-99-8

Water

IC50 = 0.20 nM

Keep at 2-10°C.

079-06133

50 mg

Highly selective serotonin receptor 5-HT3 antagonist. It is an antiemetic.

Milnacipran Hydrochloride, 98.0+ % (HPLC)

133-17011

 25 mg

for Pharmacology
Research

101152-94-7

Water

IC50 of 5-HT: 28.0 nM; NA: 29.6 nM

Keep at -20°C.

139-17013

100 mg

Serotonin-noradrenaline reuptake inhibitor (SNRI). It selectively binds to the reuptake site of serotonin and noradrenaline at nerve terminals
thus inhibiting uptake of monoamine and increasing extracellular concentrations of serotonin and noradrenaline in the brain.

Olanzapine, 98.0+ % (HPLC)

150-03071

 50 mg

for Pharmacology
Research

132539-06-1

Acetonitrile

Ki of 5-HT2A: 2.5 nM; 5-HT2B: 11.8 nM;

5-HT2C: 28.6 nM; 5-HT6: 2.5 nM;

Dopamine D2: 11 nM; Dopamine D3: 16 nM;

Dopamine D4: 27 nM; α1-adrenaline: 19 nM;
Histamine H1: 7 nM

Keep at RT.

156-03073

500 mg

Olanzapine antagonizes various neuronal receptors including serotonin 5-HT2A, 2B, 2C, 5-HT6, dopamine D2, D3, D4, α1-adrenaline,
histamine H1 receptors.

Paroxetine Hydrochloride, 98.0+ % (HPLC)

168-24431

100 mg

for Pharmacology
Research

78246-49-8

Water

IC50 = 0.29 nM

Keep below 25°C.

Potent and selective serotonin reuptake inhibitor (SSRI) in the serotonin neuron system in brain

Perospirone Hydrochloride Dihydrate, 98.0+ % (HPLC)

167-25241

 5 mg

for Pharmacology
Research

192052-81-6

Methanol, ethanol,
acetonitrile, water

5-HT2: Ki=0.61 nM; Dopamine D2: 1.4 nM

Keep at RT.

163-25243

50 mg

It binds selectively to dopamine D2 receptor and serotonin 5-HT2 receptor and exhibits antagonistic activities.

Quetiapine Fumarate, 98.0+ % (HPLC)

172-00691

 1 g

for Pharmacology
Research

111974-72-2

N,N-
Dimethylformamide

IC50 of 5-HT2: 148 nM; Dopamine D2:
329 nM; adrenaline α1: 94 nM;
Histamine H1: 30 nM

Keep at RT.

178-00693

10 g

Dibenzothiazepine compound. It inhibits dopamine D2 receptor and serotonin 5HT2 receptor. It shows affinity to a number of receptors other
than dopamine D2 and serotonin 5HT2. It shows higher affinity to serotonin 5HT2 receptor than dopamine D2 receptor.

Risperidone

188-02311

 50 mg

for Pharmacology
Research

106266-06-2

Methanol

-

Keep at RT.

184-02313

250 mg

It binds selectively to dopamine D2 receptor and serotonin 5-HT2A receptor and exhibits antagonistic activities.

Sertraline Hydrochloride, 98+ % (HPLC)

193-16191

100 mg

for Pharmacology
Research

79559-97-0

Methanol

IC50 = 0.058 μM

Keep at RT.

199-16193

1 g

Selective serotonin reuptake inhibitor (SSRI). It exhibits antidepressant activity by the inhibition of serotonin reuptake in the brain and
increase in the amount of serotonin in synaptic gaps.

Trazodone Hydrochrolide, 98.0+ % (HPLC)

209-14964

500 mg

for Biochemistry

25332-39-2

Water

IC50 of 5-HT uptake: 580 nM;
NA uptake: 11 μM

Keep at 2-10°C.

Triazolopyridine antidepressant, which acts more selectively on serotonin than on noradrenaline in its inhibition of monoamine reuptake and
exerts antidepressant activity. It has almost no anti-cholinergic effects and hardly inhibits reuptake of noradrenalin in the heart.

Venlafaxine Hydrochloride, 98.0+ % (HPLC)

227-01951

500 mg

for Pharmacology
Research

99300-78-4

Water

Ki = 41.0 ± 9.1 μM

Keep at RT.

Serotonin-noradrenaline reuptake inhibitor (SNRI). It selectively binds to the reuptake site of serotonin and noradrenaline at nerve terminals
thus inhibiting uptake of monoamine and increasing extracellular concentrations of serotonin and noradrenaline in the brain.

(6) Dopamine Receptor Antagonists

Aripiprazole, 98.0+ % (HPLC)

017-23831

100 mg

for Pharmacology
Research

129722-12-9

Benzyl alcohol,
acetic acid

IC50 = 37 nM (with 100 nM Dopamine)

Keep at RT.

013-23833

1 g

Quinoline derivative antagonist of dopamine D2 receptor when dopamine is insufficient. It also acts as partial agonist of serotonin 5-HT1A
receptor and dopamine D2 receptor and antagonist of serotonin 5-HT2A receptor.

Bupropion Hydrochloride, 98.0+ % (HPLC)

028-17311

100 mg

for Pharmacology
Research

21535-47-7

Methanol

IC50 of NA transporter: 1.4 μM;
DA transporter: 2.8 μM

Keep at RT.

024-17313

1 g

Noradrenaline-dopamine reuptake inhibitors (DNRIs).

It inhibits the reuptake of noradrenalin and dopamine into the nerve terminals in the brain, thereby increasing the extracellular serotonin
concentrations of noradrenaline and dopamin in the brain.

Clozapine, 98.0+ % (HPLC)

038-22741

10 mg

for Pharmacology
Research

5786-21-0

Ethanol

IC50 of D4: 9 nM; 5-HT2A: 12 nM;
5-HT2C: 8 nM

Keep at RT.

034-22743

50 mg

Subtype D4 selective dopamine receptor antagonist. It also antagonizes serotonin receptors (5-HT2A, 5-HT2C, 5-HT3, 5-HT6, 5-HT7).

Haloperidol, 98.0+ % (Titration)

084-04261

 1 g

Wako Special Grade

52-86-8

Acetic acid, glacial,
chloroform

-

Keep at RT.

080-04263

 5 g

082-04262

25 g

Haloperidol antagonizes especially dopamines at the dopamine receptor and blocks their action.

(+)-SCH23390 Hydrochloride, 98.0+ % (HPLC)

191-15531

10 mg

for Cellbiology

125941-87-9

DMF

IC50 of D1: 0.2 nM; D5: 0.3 nM

Keep at 2-10°C.

197-15533

50 mg

Potent dopamine D1 receptor antagonist. It also potently agonizes 5-HT1C/2C receptors.

(±)-Sulpiride, 98.0+ % (Titration)

190-12061

  1 g

for Biochemistry

15676-16-1

Acetic acid, glacial

D2: IC50 = 4 nM

Keep at 2-10°C.

198-12062

 25 g

196-12063

100 g

This product blocks dopamin D2 receptors, thereby increasing the extracellular dopamine levels in the brain. It exhibits little antagonist
action on the receptors of monoamine such as adrenaline and serotonin.

(7) Noradrenaline-related Inhibitors

Maprotiline Hydrochloride, 98.0+ % (HPLC)

139-17091

1 g

for Pharmacology
Research

10347-81-6

Methanol,
chloroform

IC50 = 8.4 nM

Keep at RT.

135-17093

5 g

Tetracyclic antidepressant. It increases noradrenaline concentrations by inhibiting the reuptake of noradrenaline into the nerve terminals.

Mianserin Hydrochloride

132-16861

 50 mg

for Pharmacology
Research

21535-47-7

Methanol

IC50 of α2 adrenaline receptor: 12 nM;
α adrenaline receptor: 300 nM;
5-HT receptor: 22 nM

Keep at RT.

138-16863

500 mg

Tetracyclic antidepressant. It blocks presynaptic α2 adrenaline autoreceptor, thereby accelerates noradrenaline release into synaptic gaps.
Acceleration of metabolic turnover of noradrenaline in the brain has also been reported. It exhibits 5-HT receptor blocking activity.

Mirtazapine, 98.0+ % (HPLC)

134-16821

10 mg

for Pharmacology
Research

85650-52-8

Ethanol, methanol,
chloroform

pKi = 6.9 - 7.0 (α2); 5.2 (5-HTA1);

7.88 (5-HT2); 6.8, 8.1 (5-HT3);

5.5 - 5.8 (NA uptake); <5.0 (5-HT uptake)

Keep at RT.

130-16823

50 mg

Noradrenergic and specific serotonergic antidepressant. Mirtazapine acts as an antagonist on presynaptic α2-adrenergic autoreceptors and
heteroreceptors and enhances noradrenaline and serotonin (5-HT) releases and adrenergic and serotonergic neurotransmission in the brain.
It also blocks 5-HT2 and 5-HT3 receptors and selectively activates 5-HT1A receptors.

(8) Alzheimer's Disease Research

BMS 299897, 97.0+ % (HPLC)

021-17781

 5 mg

for Cellbiology

290315-45-6

-

-

Keep at -20°C.

027-17783

25 mg

Potent γ-secretase inhibitor that inhibits the formation of the amyloids Aβ40 and Aβ42 in vitro. It is also known not to inhibit Notch signaling.
It has oral activity.

DAPT, 97.0+ % (HPLC)

045-30981

 5 mg

for Cellbiology

208255-80-5

Methanol

-

Keep at -20°C.

041-30983

25 mg

γ-secretase inhibitor.

Donepezil Hudrochloride, 90.0+ % (HPLC)

045-32321

 50 mg

for Biochemistry

120011-70-3

Water (1 mg/mL)

-

Keep at 2-10°C.

041-32323

250 mg

Reversible acetylcholinesterase (AChE) inhibitor. Donepezil-induced downregulation of AChE leads to increased levels of acetylcholine in the
brain, which in turn stimulates cholinergic nerve system in the brain.

L-685, 458, 98.0+ % (HPLC)

121-06141

1 mg

for Cellbnioloty

292632-98-5

DMSO (>10 mg/mL)

-

Keep at -20°C.

Potent and selective γ-secretase inhibitor. It also inhibits with equal potency to Aβ40 and Aβ42 peptides.

indexpage top

index

A
A-83-01 AACOCF317-AAGAG 1296AG 1478AG 490ω-Agatoxin IVAω-Agatoxin TKAgeleninAlendronate Sodium Salt TrihydrateALK5 InhibitorAM 251AM 281AM 630AMG 9810DL-2-Amino-4-phosphonobutyric AcidL-2-Amino-4-phosphonobutyric AcidD(-)-2-Amino-5-phosphonovaleric AcidDL-2-Amino-5-phosphonovaleric AcidAminogenisteinAmitriptyline HydrochlorideAmlodipineAmoxapineAndrographolideAP 18Apamin2-APBAPETx2ApigeninAripiprazoleAS 604850AS 6 05240ATM Kinase InhibitorAzasetron Hydrochloride
B
BAY 11-7085BCTCBenazepril Hydrochloride(+)-Bicuculline(-)-Bicuculline Methobromide (-)-Bicuculline MethochlorideBio(-)-BlebbistatinBlonanserinBMS 2998976-Bromoindirubin-3'-oximeBupropion Hydrochloride2,3-Butanedione Oxime Butein
C
CalcicludineCalciseptine Calpain Inhibitor 2Calphostin CCalyculin ACantharidin CapsazepineCaptoprilCarbonyl Cyanide m-ChlorophenylhydrazoneCharybdotoxinDL-p-Chlorophenylalanine8-(4-Chlorophenylthio)adenosine 3',5'-(Cyclic)monophosphate Sodium SaltChlorotoxinChlorpromazine HydrochlorideCinnarizineCitalopram HydrobromideCKI-7 DihydrochlorideClomipramine HydrochlorideClotrimazoleClozapineCompound 15eCompound 401α-Conotoxin G1μ-Conotoxin G3Bμ-Conotoxin GSω-Conotoxin GVIA α-Conotoxin ImIα-Conotoxin M1ω-Conotoxin MVIIAω-Conotoxin MVIIC α-Conotoxin SIμ-Conotoxin SIIIAω-Conotoxin SVIB (R)-CPPCurcumin Cyclopiazonic AcidCyclosporin A
D
D-AP5DL-AP5DAPTDeguelinDendrotoxin 1Desipramine HydrochlorideDextromethorphan Hydrobromide MonohydrateDiazoxideDibucaine HydrochlorideDiltiazem HydrochlorideDisodium β-Glycerophosphate Pentahydrate2,5-Di-t-butylhydroquinoneDL-AP7DNQXDonepezil HudrochlorideDorsomorphinDorsomorphin DihydrochlorideDoxepin HydrochlorideDuloxetine Hydrochloride
E
E-4031 n-HydrateE-64dEnalaprilat DihydrateEnalapril MaleateEvans Blue
F
Felbamate(±)-Fluoxetine HydrochlorideFluphenazine DimaleateFluvoxamine Maleate Fostriecin Sodium Salt
G
GeldanamycinGenisteinGenistinGF 109203XGlibenclamideGo 6983Granisetron HydrochlorideGSK-3 Inhibitor IXGSK 269962AGSK 429286AGsMTx-4Guangxitoxin-1E
H
H-1152 DihydrochlorideHaloperidolHC-030031Herbimycin AHuwentoxin-IVHypericin
I
IberiotoxinIPA-3Isotetrandrine
J
Joro Spider Toxin JSTX-3
K
K-252aK-252bKaliotoxin (1-37)KenpaulloneKi 8751KN-62KN-93KN-93, Water-SolubleKT 5720KT 5823KU 0063794Kurtoxin
L
L-685, 458LDN 193189 HydrochlorideLevamisole HydrochlorideLisinopril DihydrateLoperamide Hydrochloride LY-83583LY 294002Lys-Lys-Lys-Leu-Arg-Arg-Gln-Glu-Ala-Phe-Asp-Ala-Tyr
M
Maprotiline HydrochlorideMargatoxin Mastoparan MCD-Peptide(+)-MCPGMemantine Hydrochloride 3-MethyladenineMG-132MgTXMianserin Hydrochloride Milnacipran HydrochlorideMirtazapine(+)-MK 801 Maleate
N
NBQXNBQX Disodium SaltNicardipine HydrochlorideNitrendipineNS2028NSC 693868NU 7026NU 7441
O
ODQOlanzapineOlomoucineOlvanilOmeprazole1H-[1,2,4]Oxadiazolo[4,3-a]quinoxalin-1-one
P
Paroxetine HydrochloridePD-98059PD 173074PD 184352PD 0325901Pentamidine IsethionatePentoxifyllinePerospirone Hydrochloride DihydratePhloretinPhosphatase Inhibitor Cocktail Solution I Phosphatase Inhibitor Cocktail Solution II PI-103PiceatannolPicrotoxinPicrotoxininPIK-75 HydrochloridePKC 412PLTX-IIPP 2PP 3PP 242Protease Inhibitor Cocktail Set IProtease Inhibitor Cocktail Set IIIProtease Inhibitor Cocktail Set IIIProtease Inhibitor Cocktail Set IVProtease Inhibitor Cocktail Set V Protease Inhibitor Cocktail Set VIProtease Inhibitor Cocktail Set VIIProTx-1ProTx-IIPsalmotoxin 1Purotoxin-1
Q
Quercetin DihydrateQuetiapine FumarateQuinacrine Dihydrochloride Dihydrate
R
Rac1 InhibitorRadicicolRapamycin RG-14620Risperidone RK-682RN-1747Ro 31-8220 MethanesulfonateRolipramRoscovitineRuthenium RedRyanodine
S
SB 202190SB 203580SB 203580 HydrochlorideSB-366791SB 415286SB 431542(+)-SCH23390 HydrochlorideScyllatoxinSertraline HydrochlorideSNX-482SP 600125SpermineD-erythro-SphingosineSR 3677 HydrochlorideStaurosporineStellettamide A TrifluoroacetateStichodactyla ToxinSU 4312SU 5402SU 5416SU 6668SU 11274(±)-SulpirideSuramin Sodium
T
Tamoxifen CitrateTautomycinTertiapinTGF-β R I Kinase Inhibitor IVThapsigargin Tityustoxin KαTrazodone HydrochrolideTriciribineTWS 119Tyrphostin A25
U
U 0126
V
Venlafaxine HydrochlorideVerapamil Hydrochloride
W
W-5 HydrochlorideW-7 Hydrochloride(+)-Wortmannin
Y
Y-276325 mmol/L Y-27632 Solution
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