EPZ005687是一种有效的,选择性EZH2抑制剂,Ki为24 nM,比作用于EZH1选择性高50倍,比作用于15种其他蛋白甲基转移酶选择性高500倍。;EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases
参考文献:
1. Knutson SK, et al. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol. 2012;8(11):890-6. 2. Tang SH, et al. Effects of H3K27 methylation inhibitor EPZ005687 on apoptosis, proliferation and cell cycle of U937 cells and normal CD34 positive cells. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2014 Dec;22(6):1561-6.