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Tenovin-1

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.

Product Specifications

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.

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)

Molecular Formula

C20H23N3O2S

Shipping Conditions

Room Temperature (continental US) or Gel Packs

Storage Conditions

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.

Calculated Molecular Weight

369.5 Da

CAS Number

380315-80-0

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