TENOVIN-1

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 .

MDM-2/p53; DHODH; Sirtuin

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[5] CHRISTIAN MARX. The sirtuin 1/2 inhibitor tenovin-1 induces a nonlinear apoptosis-inducing factor-dependent cell death in a p53 null Ewing’s sarcoma cell line.[J]. Investigational New Drugs, 2018: 396-406. DOI:10.1007/s10637-017-0541-1
[6] MINJI BANG. Tenovin-1 Induces Senescence and Decreases Wound-Healing Activity in Cultured Rat Primary Astrocytes.[J]. Biomolecules & Therapeutics, 2019, 27 3: 283-289. DOI:10.4062/biomolther.2018.107