WM-1119

Description: WM-1119 is a novel, highly potent, and selective inhibitor of KAT6A/B (lysine acetyltransferase) with an IC50 value of of 0.25 uM for KAT6A, KD value of 2 nM for KAT6A, KD value of 2.2 uM for KAT5, and KD value of 0.5 uM for KAT7. WM-1119 induces cell cycle exit and cellular senescence without causing DNA damage. Senescence is INK4A/ARF-dependent and is accompanied by changes in gene expression that are typical of loss of KAT6A function. WM-1119, which has increased bioavailability, arrests the progression of lymphoma in mice. We anticipate that this class of inhibitors will help to accelerate the development of therapeutics that target gene transcription regulated by histone acetylation.

References: Nature. 2018 Aug; 560(7717):253-257.