| 货号 | 66244S |
| 供应商 | CST |
| 背景 | GSK343 inhibits EZH2 and EZH1 histone-lysine N-methyltransferase activity through competitive inhibition of the cofactor S-Adenosyl-l-methionine (SAM). IC50 values for EZH2 and EZH1 are 4 nM and 60 nM, respectively (1). Research studies show that GSK343 displays more than 1000-fold selectivity relative to other methyltransferases (1,2). These studies demonstrate that GSK343 induces cancer cell autophagy and enhances the anti-cancer effects of the multi-kinase inhibitor, sorafenib (3). |
| 存放说明 | -20C |
| 参考文献 | 1 . Konze, K.D. et al. (2013) ACS Chem Biol 8, 1324-34. 2 . Amatangelo, M.D. et al. (2013) Cell Cycle 12, 2113-9. 3 . Liu, T.P. et al. (2015) Anticancer Drugs 26, 139-47. |
Chemical structure of GSK343. | |
Western blot analysis of extracts from HeLa cells, untreated (-) or treated with GSK343 (48 hr) at the indicated concentrations, using Tri-Methyl-Histone H3 (Lys27) (C36B11) Rabbit mAb #9733 (upper) and Histone H3 (D1H2) XP® Rabbit mAb #4499 (lower). |
