Tenovin-1
Catalog #
27660-1
$155
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Description
Tenovin-1 inhibits the protein-deacetylating activities of SIRT1 and SIRT2. Tenovin-1 is also a p53 activator and elevates the amount of p53 protein within 2 hr of treatment, without altering p53 mRNA levels. Tenovin-1 protects against MDM2-mediated p53 degradation via ubiquitination.
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Synonyms
N-[(4-acetamidophenyl)carbamothioyl]-4-tert-butylbenzamide
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Product Data Gallery
Product Info
Storage and Usage
Citations
Purity
≥99% by HPLC
Target(s)
SIRT1, SIRT2
Formula
C20H23N3O2S
MW
369.5 Da
Solubility
Soluble in DMSO 74 mg/ml (200 mM), or 15% Captisol (modified cyclodextrin) 15 mg/ml. Solubility in water or ethanol is < 1 mg/ml (< 1 mM)
CAS Registry #
380315-80-0
Background
Tenovin-1, a small molecule discovered by a cell-based screen, is a bio-active activator of p53 that elevates the levels of p53 protein, p53-downstream target p21CIP/WAF1 protein and mRNA and protects p53 from mdm2-mediated degradation with little impact on p53 synthesis. Tenovin-1 also exerts inhibition against human sirtuin 1 (SIRT1) and sirtuin 2 (SIRT2), two important members of the sirtuin family. Tenovin-1 represses cell growth, and induces apoptosis in a panel of tumor cells expressing p53. An improved and water-soluble version of tenovin-1 has been found to decrease the peptide deacetylase activity of human SIRT1 and SIRT2 with IC50 values of 21 µM and 10 µM respectively.
References
Lain S, et al. Cancer Cell. 2008 May;13(5):454-63.
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