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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator.
Lain S, et al. Cancer Cell. 2008 May;13(5):454-63. PMID: 18455128.
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