Biochem/physiol Actions
Potent and selective, acetyl-CoA-competitive MYST family histone acetyltransferases KAT6A and KAT6B inhibitor with anti-cancer efficacy in vitro and in vivo.
WM-1119 is a potent and selective, acetyl coenzyme A (Acetyl-CoA)-competitive inhibitor against MYST family histone acetyltransferases KAT6A and KAT6B (KAT6B Kd = 2.1 nM by SPR, IC50 = 37 nM by activity assay; KAT7/5 Kd = 0.53/2.2 μM; no affinity toward 159 diverse biological targets). WM-1119 induces MEF G1 cell cycle arrest (1-10 μM), inhibits EMRK1184 lymphoma growth in cultures (IC50 = 250 nM) and in mice in vivo (50 mg/kg 3x or 4x i.p. per day).