8. Physiological Active Substances

Akt (Protein Kinase B; PKB) inhibitor
Deguelin
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Wako Cat. No. 047-29211 (5 mg) <for Cellbiology>
Keep at 2~10℃


It inhibits proliferation of cells in the GM-2 stage of cell cycle. It induces apoptosis in the precancerous and cancerated cell lines. The derris root, a legume growing naturally in the South Seas and the tropics, contains a highly potent ingredient lethal to fi sh and insects. This is an analogue of the active component , rotenone.

Appearance:Slightly pale yellow ~ yellow, crystalline powder ~ powder
Solubility: Soluble in acetone, dichloromethane, acetonitrile and DMSO.
[References]
1) Chun, K. H., et al.: "Eff ects of deguelin on the phosphatidylinositol 3-kinase/Akt pathway and apoptosis in premalignant human bronchial epithelial cells", J. Natl. Cancer Inst., 95, 291-302 (2003)
2) Ito, C., et. al.: "Cancer chemopreventive activity of rotenoids from Derris trifoliata", Planta Med., 70, 8-11 (2004)
Marine Natural Products -- Protein Phosphate Inhibitor
Dinophysistoxin-I [DTX-I]
Wako Cat. No. 042-28661 (100 µg) <for Biochemistry>
Keep at 2~10℃


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Dinophysistoxin, isolated from Halichondria okadai, is a diarrhetic shellfi sh toxin with 35-methyl okadaic acid. Dinophysistoxin-1 is a potent Non-TPA* type tumor promoter and specifi cally inhibits protein phosphatases.
*TPA: 12-o-Tetradecanoyl-phorbol-13-acetate
Source:Halichondria okadai
Appearance: film
Solubility:Soluble in methanol, ether, acetone, ethyl acetate and chloroform.
[References]
Suganuma, M., Fujiki, H., Suguri, H., Yoshizawa, S., Hirota, M., Nakayasu, M., Ojika, M., Wakamatsu, K., Yamada, K. and Sugimura, T.: "Okadaic acid: an additional nonphorbol- 12-tetradecanoate-13-acetate-type tumor promoter", Proc. Natl. Acad. Sci. USA, 85, 1768 -71 (1988).
HSP60 Inhibitor
ETB [Epolactaene Tertiary Butyl Ester] (mixture of isomers)
Wako Cat. No. 051-07671 (200 µg) <for Cellbiology>
Keep at -20℃


Wako has launched a new inhibitor which were discovered by Dr. Hiroyuki Osada, Antibiotics laboratory of Institute of Physical and Chemical Research (RIKEN) under license from RIKEN.
This product is a derivative of epolactaene isolated from Penicillium. It has a more potent cytostatic effect on human neuroblastoma cells SH-SY 5Y than that of epolactaene, and induces apoptosis. Furthermore, it has been revealed that ETB induces apoptosis in human T-lymphoma cells Jurkat. Recently, HSP60 was identifi ed as one of ETB binding proteins. ETB binds to HSP60 to inhibit chaperone activity.
Appearance: White ~ slightly pale brown, crystalline powder ~ powder
Solubility: Soluble in methanol (1 vial is dissolved with 0.2 mL of methanol).
[References]
Nagumo, Y., Kakeya, H., Shoji, M., Hayashi, Y., Dohmae, N. and Osada, H.: "Epolactaene binds human Hsp60 Cys442 resulting in the inhibition of chaperone activity", Biochem. J., 387(3), 835-40 (2005).
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Wako Product Update Bio-No.1 [ page. 28 ]