Background:

BRD4770 is a novel G9a(EHMT2) inhibitor with EC50 of 5 uM (trimethylated H3K9 in PANC-1 cell).IC50 value: 5 uM (PANC-1 cell) [1]Target: G9a inhibitorBRD4770 activates the ATM pathway without inducing DNA damage, while the ATR pathway is not affected. BRD4770 is a novel probe for studying G9a and its role in cellular senescence.Treatment of 5 μM BRD4770 for 24 h decreased H3K9 trimethylation level by 23% in PANC-1 cells. BRD9539 also inhibits PRC2 activity.

参考文献:
[1]. Yuan Y, et al. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma. ACS Chem Biol. 2012 Jul 20;7(7):1152-7.