Tenovin-1 is a small molecule activator of p53 transcriptional activity. At 10 µM, it elevates p53 expression in MCF-7 cells within two hours of treatment and longer-term exposure significantly decreases the growth of BL2 Burkitt’s lymphoma and ARN8 melanoma cells.1 Functioning upstream of p53, tenovin-1 acts by inhibiting the deacetylase activity of purified human SIRT1 and SIRT2, members of NAD+-dependent class III histone deacetylases that belong to the sirtuin family.1 While tenovin-1 demonstrates low genotoxicity, the compound has poor water solubility, which limits its uses in vivo.
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