一般描述
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.
生化/生理作用
Cell permeable: no
Primary Target
PMA-induced skin thickening
Product does not compete with ATP.
Reversible: no
Target IC50: 210-470 nM against Dnmt1; 30, 50, 60 and 70 µM for p300, CBP, PCAF and TIP60
包装
Packaged under inert gas
重悬
Following reconstitution, aliquot and freeze at -20°C. DMSO stock solutions are stable for up to 3 months at -20°C.
其他说明
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany