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. 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. While tenovin-1 demonstrates low genotoxicity, the compound has poor water solubility, which limits its uses in vivo.
Tenovin 1 is a sirtuin inhibitor.
ChEBI: N-[(4-acetamidoanilino)-sulfanylidenemethyl]-4-tert-butylbenzamide is a member of thioureas.
p53 activator that protects against MDM2-mediated p53 degradation. Elevates levels of p53 and p21 CIP/WAF1 and induces expression from an endogenous p53-dependent promoter. Exhibits potent antiproliferative activity in vitro .
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