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Identification of a cell-active non-peptide sirtuin inhibitor containing N-thioacetyl lysine

Identification of a cell-active non-peptide sirtuin inhibitor containing N-thioacetyl lysine

Bioorganic and Medicinal Chemistry Letters 19(19): 5670-5672

To identify cell-active sirtuin inhibitors containing N-thioacetyl lysine, we synthesized compound 1, which was designed based on the structure of the reported N-ethoxycarbonylacetyl lysine-based sirtuin inhibitor NCS-12k. Compound 1 selectively inhibited SIRT1 in enzyme assays. Compound 1 also caused a dose-dependent increase in p53 acetylation in human colon cancer HCT116 cells, indicating the inhibition of SIRT1 in these cells.

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Accession: 053660498

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PMID: 19700324

DOI: 10.1016/j.bmcl.2009.08.028

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