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Tenovin-1, a small molecule discovered by a cell-based screen, is a bio-active activator of p53 that elevates the levels of p53 protein, p53-downstream target p21CIP/WAF1 protein and mRNA and protects p53 from mdm2-mediated degradation with little impact on p53 synthesis. Tenovin-1 also exerts inhibition against human sirtuin 1 (SirT1) and sirtuin 2 (SirT2), two important members of the sirtuin family. Due to its insufficient solubility, an improved and water-soluble version of tenovin-1 has been found to decrease the peptide deacetylase activity of human SirT1 and SirT2 with values of 50% inhibition concentration IC50 of 21 μM and 10 μM respectively.

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