BRD4770 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2), also known as G9a, decreasing di- and trimethylation on lysine 9 of histone 3 (EC50 = 5 μM). Through its effects on EHMT2, BRD4770 induces senescence in the pancreatic cancer cell line PANC-1 without initiating apoptosis. It also blocks both anchorage-dependent and –independent proliferation of PANC-1 cells.[Cayman Chemical]
Biochem/physiol Actions
BRD4770 is a selective inhibitor of the histone methyltransferase G9a. BRD4770 blocks lysine residue 9 methylation of histone H3 without inducing apoptosis. In PANC-1 cells, BRD4770 activates the ataxia telangiectasia mutated (ATM) pathway, induces senescence and inhibits anchorage-dependent and -independent growth.
