UNC0646

基本信息

半岛bd体育手机客户端 描述

UNC0646 is a potent and selective G9a inhibitor with IC50 of 6 nM. IC50 value: 6 nM [1] Target: G9a UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50 values are 6 nM and 15 nM for G9a and GLP, respectively). UNC0646 potently blocks G9a/GLP methyltransferase activity in cells (IC50 = 10 nM in MCF7 cells); exhibits low cellular toxicity (EC50 = 4.7 μM in MCF7 cells). UNC0646 is selective for G9a/GLP over a range of other protein lysine methyltransferases and protein arginine methyltransferases.

参考文献

[1]. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50.