2. Academic Validation
  3. Identification of KD5170: a novel mercaptoketone-based histone deacetylase inhibitor

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

  • Bioorg Med Chem Lett. 2008 Dec 1;18(23):6093-6. doi: 10.1016/j.bmcl.2008.10.029.
Joseph E Payne 1,  Céline Bonnefous,  Christian A Hassig,  Kent T Symons,  Xin Guo,  Phan-Manh Nguyen,  Tami Annable,  Paul L Wash,  Timothy Z Hoffman,  Tadimeti S Rao,  Andrew K Shiau,  James W Malecha,  Stewart A Noble,  Jeffrey H Hager,  Nicholas D Smith
Affiliations

Affiliation

  • 1 Department of Chemistry, Kalypsys, Inc., 10420 Wateridge Circle, San Diego, CA 92121, USA.
PMID: 18954983 DOI: 10.1016/j.bmcl.2008.10.029
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 i.v. dose and inhibition of tumor growth following chronic dosing.

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