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

  title={Identification of KD5170: a novel mercaptoketone-based histone deacetylase inhibitor.},
  author={Joseph E Payne and C{\'e}line Bonnefous and Christian A. Hassig and Kent T Symons and Xin Yong Guo and Phan-Manh Nguyen and Tami Annable and Paul L Wash and Timothy Z Hoffman and Tadimeti S. Rao and Andrew K. Shiau and James W Malecha and Stewart A. Noble and Jeffrey H. Hager and Nicholas D. Smith},
  journal={Bioorganic & medicinal chemistry letters},
  volume={18 23},
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 i.v. dose and inhibition of tumor growth following chronic dosing.