Identification of KD5170: a novel mercaptoketone-based histone deacetylase inhibitor.

Abstract We report the identification of KD5170, a potent mercaptoketone-based Class I and II-histone deacetylase inhibitor that demonstrates broad spectrum cytotoxic activity against a range of human tumor-derived cell lines. KD5170 exhibits robust and sustained histone H3 hyperacetylation in HCT-116 xenograft tumors following single oral or iv dose and inhibition of tumor growth following chronic dosing.