Tenovin-1

Tenovin-1 is a p53 activator and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 induces expression from an endogenous p53-dependent promoter. Tenovin-1 exhibits potent antiproliferative activity in vitro. Tenovin-1 (10μM) 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. Tenovin-1 has been shown to activate and elevate acetylated p53 levels, induce apoptosis in vitro, and acetylate histone H4. While tenovin-1 demonstrates low genotoxicity, the compound has poor water solubility, which limits its uses in vivo.