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WM-1119 is an orally bioavailable inhibitor of lysine acetyltransferase 6A (KAT6A/MOZ; IC50 = 6.3 nM).1 It binds to KAT6A with a Kd value of 2 nM and is selective for KAT6A over KAT5 and KAT7 (Kds = 2,200 and 500 nM, respectively), as well as over a panel of 159 additional targets at 1 and 10 μM.2 WM-1119 inhibits proliferation of EMRK1184 B cell lymphoma cells (IC50 = 0.25 μM). It reduces tumor growth and spleen weight in a murine EMRK1184 model when administered at a dose of 50 mg/kg four times per day. See the Structural Genomics Consortium (SGC) website for more information.
WARNING This product is not for human or veterinary use.
1. Discovery of acylsulfonohydrazide-
2. Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth. Nature 560(7717), 253-257 (2018).