Background
BRD9539 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2), also known as G9a, with an IC50 value of 6.3 ?M.1 It inhibits polycomb repressive complex 2 (PRC2) to a similar extent with 54 and 43% activity remaining for G9a and PRC2, respectively, when used at a concentration of 10 ?M. It is selective for G9a and PRC2 over SU39H1 and NDMT1 up to a concentration of 40 ?M. It is more potent than BRD4770 in enzyme assays but has no activity in cell-based assays when used at concentrations of 5 and 10 ?M.
1.Yuan, Y., Wang, Q., Paulk, J., et al.A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinomaACS Chem. Biol.7(7)1152-1157(2012)
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