Description
Tenovin-1 protects against MDM2-mediated p53 degradation, which involves ubiquitination, and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2.
Storage
2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.
Molecular Formula
C20H23N3O2S
Chemical Name
Benzamide, N-[[[4-(acetylamino)phenyl]amino]thioxomethyl]-4-(1,1-dimethylethyl)-
Solubility
DMSO 74 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL
In vitro
Tenovin-1 is a p53 activator and elevates the amount of p53 protein within 2 hr of treatment. Tenovin-1 treatment does not alter p53 mRNA levels. Tenovin-1 (10μM) protects p53 from mdm2-mediated degradation with little effect on p53 synthesis. Tenovin-1 represses cell growth, and induces apoptosis in a panel of tumor cells expressing p53. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2, two important members of the sirtuin family.
In vivo
Initial in vivo experiments indicated that tenovin-1 impairs the growth of BL2-derived tumor xenografts.
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