Biochem/physiol Actions

Cell permeable: no

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 210-470 nM against Dnmt1; 30, 50, 60 and 70 µM for p300, CBP, PCAF and TIP60

Primary TargetPMA-induced skin thickening

General description

One of the main polyphenolic constituents of green tea that exhibits potent antitumor, anti-inflammatory, and antioxidant properties. Arrests cell cycling at G₀/G₁ phase and induces apoptosis in a dose-dependent manner. Shown to inhibit PMA-induced skin thickening and to activate of protein kinase C. Also activates ornithine decarboxylase and interleukin-1α mRNA and protein expression. Acts as an inhibitor of inducible nitric oxide synthase (iNOS) gene expression and enzyme activity. Also blocks peroxynitrite-mediated formation of 8-oxodeoxyguanosine and 3-nitrotyrosine. Strongly and directly inhibits telomerase in cell-free systems and in cancer cell lines. An inhibitor of Dnmt1 (IC₅₀ = 210-470 nM). Acts as a selective and noncompetitive inhibitor of HAT activities (IC₅₀ = 30, 50, 60 and 70 µM for p300, CBP, PCAF and TIP60) with minimal effects on HDAC, SIRT and HMTase.

One of the main polyphenolic constituents of green tea that possesses potent antitumor, anti-inflammatory, and antioxidant properties. EGCG has been shown to inhibit PMA-induced skin thickening, activation of protein kinase C, activation of ornithine decarboxylase, and activation of interleukin-1α mRNA and protein expression. Has also been shown to inhibit inducible nitric oxide synthase (iNOS) gene expression and enzyme activity and to inhibit the peroxynitrite-mediated formation of 8-oxodeoxyguanosine and 3-nitrotyrosine. Also strongly and directly inhibits telomerase. Acts as a selective and noncompetitive inhibitor of HAT activities (IC₅₀ = 30, 50, 60 and 70 µM for p300, CBP, PCAF and TIP60) with minimal effects on HDAC, SIRT and HMTase.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Choi, K.C., et al. 2009. Cancer Res.69, 583.Dell′Aicia, I., et al. 2004. EMBO reports 5, 1.Tachibana, H., et al. 2004. Nat. Struct. Mol. Biol.11, 380.Naasami, I., et al. 1998. Biochem. Biophys. Res. Commun. 249, 391.Ahmad, N., et al. 1997. J. Natl. Cancer89, 1881.Chan, M.M.-Y., et al. 1997. Biochem. Pharmacol. 54, 1281.Lin, Y.-L., and Lin, J.-K. 1997. Mol. Pharmacol. 52, 465.Fiala, E.S., et al. 1996. Experientia 52, 922.Katiyar, S.K., et al. 1995. J. Invest. Dermatol. 105, 394.Liao, S., et al. 1995. Cancer Lett. 96, 239.Yamane, T., et al. 1995. Cancer Res. 55, 2081.Huang, M.T., et al. 1992. Carcinogenesis 13, 947.

Packaging

Packaged under inert gas

10 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze at -20°C. DMSO stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Irritant (B)