Background:

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 IC₅₀of 21 μM and 10 μM respectively.

Reference

?[1].Lain S, Hollick JJ, Campbell J, Staples OD, Higgins M, Aoubala M, McCarthy A, Appleyard V, Murray KE, Baker L, Thompson A, Mathers J, Holland SJ, Stark MJ, Pass G, Woods J, Lane DP, Westwood NJ. Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator. Cancer Cell. 2008 May;13(5):454-63. doi: 10.1016/j.ccr.2008.03.004.