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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.
CAS Number: 380315-80-0
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.
Purity: ≥99% by HPLC
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)
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: SIRT1, SIRT2
Biosafety Level: Not applicable (BSL-1)
References: Lain S, et al. Cancer Cell. 2008 May;13(5):454-63.
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