KAT6 inhibitor MEN2312

An orally bioavailable inhibitor of MYST histone acetyltransferase (HAT) KAT6, with potential antineoplastic activity. Upon oral administration, KAT6 inhibitor MEN2312 targets and binds to KAT6, and inhibits the acetylation of histones and other nonhistone substrates. This may disrupt gene expression and inhibit the proliferation of tumors that overexpress KAT6. KAT6A (MOZ; MYST3) and KAT6B (MORF; MOZ2; MYST4), commonly amplified genes in solid tumors, play key roles in cell cycle regulation and in tumorigenesis.