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  • Title: Identification of KD5170: a novel mercaptoketone-based histone deacetylase inhibitor.
    Author: Payne JE, Bonnefous C, Hassig CA, Symons KT, Guo X, Nguyen PM, Annable T, Wash PL, Hoffman TZ, Rao TS, Shiau AK, Malecha JW, Noble SA, Hager JH, Smith ND.
    Journal: Bioorg Med Chem Lett; 2008 Dec 01; 18(23):6093-6. PubMed ID: 18954983.
    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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