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8. Physiological Active Substances

Histone Deacetylase (HDAC) Inhibitor
Trichostatin A, 99.0+ % (HPLC)
Wako Cat. No. 200-11993 (1 mg); 204-11991 (5 mg) <for Biochemistry >
Keep at -20℃

HDAC plays a central role in chromatin structure formation associated with the nuclear distribution of DNA. There are presently 17 known types of this enzyme in mammals, which are classifi ed into 3 classes. Also, HDAC Class III has been reported to be associated with regulation of aging and life span.
HDAC inhibitors show connections with cell division cycles and differentiation, as well as with antitumor activity and apoptosis-inducing activity through the inhibition of the deacetylating activity of HDAC. They can be used for studies on cellular functions involving histone deacetylase.
Trichostatin A (TSA), a Streptomyces product, specifi cally inhibits the cell cycle of normal rat fi broblasts in the G1 and G2 phases at very low concentrations as reported by Yoshida, et al. TSA-induced G2-arrest induces the formation of proliferative tetraploid cells. In addition, nanomolar concentration of TSA has been shown to cause an accumulation of highly acetylated histones in vivo, and markedly inhibit the activity of partially purifi ed histone deacetylase in vitro.
TSA appears to be a useful product for researching the multiple functions of histone acetylation in regulatory mechanisms of eukaryotic cell proliferation and differentiation.

Source: Streptmyces Hygroscopicus
Solubility: Soluble in ethanol and acetone. 1 mg/10 mL (methanol)
1) Yoshida, M., Beppu, T.: "Reversible arrest of proliferation of rat 3Y1 fi broblasts in both the G1 and G2 phases by trichostatin A", Exp. Cell. Res., 177, 122-31 (1988)
2) Yoshida, M. et al.: "Potent and specifi c inhibition of mammalian histone deacetylase both in vivo and in vitro by trichostatin A", J. Biol. Chem., 265, 17174-9 (1990)
3) Dion, L.D. et al.: "Amplifi cation of recombinant adenoviral transgene products occurs by inhibition of histone deacetylase", VIROLOGY, 231, 201-9 (1997)
Cell Cycle Inhibitor
Tryprostatin A, from Xaspergillus fumigatus BM939
Wako Cat. No. 203-16961 (500 µg) <for Cellbiology>
Keep at -20℃, Lyophilized film

Tryprostatin A (TPS-A) is an alkaloid antibiotic isolated from Aspergillus. It affects the microtubule-associated protein binding site and exhibits antitumor activity by inhibition of cell cycle progression in the M phase specifi cally.
This product was discovered by Dr. Hiroyuki Osada, Antibiotics laboratory of Institute of Physical and Chemical Research (RIKEN, Japan).

Source: Streotomyces spiroverticillatus
Solubility: Soluble in ethanol. Practically insoluble in water.
Usui T, Kondoh M, Cui CB, Mayumi T, Osada H.: "Tryprostatin A, a specifi c and novel inhibitor of microtubule assembly", Biochem J., 333, 543-8 (1998).

Membrane-Permeable Inhibitor of IP3 Receptor
Xestospongin C, from Xestospongia sp., 90+% (HPLC)
Wako Cat. No. 244-00721 (100 µg) <for Cellbiology>
Keep at -20℃, Lyophilized form in 20 mmol/L HEPES solution (pH 7.3) containing 0.1 % BSA as a stabilizer, packaged under inert gas.

A selective and membrane-permeable inhibitor of the inositol 1,4,5-triphophate (IP3) receptor-mediated Ca2+ release, isolated from an Okinawan marine sponge Xestospongia sp. A potent and highly sensitive inhibitor of IP3 receptor with IC50 of 350 nM, which is 30 times lower than that for ryanodine-receptor.

Miyamoto, S., et al., "Xestospongin C, a selective and membrane-permeable inhibitor of IP3 receptor, attenuates the positive inotropic eff ect of A-adrenergic stimulation in guinea-pig papillary muscle", Br J Pharmacol. 130, 650-4 (2000).

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Wako Product Update Bio-No.1 [ page. 35 ]