Tenovin-1 is a p53 activator and acts through inhibition of protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 induces expression from an endogenous p53-dependent promoter. Tenovin-1 exhibits potent antiproliferative activity in vitro. Tenovin-1 (10μM) 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. Tenovin-1 has been shown to activate and elevate acetylated p53 levels, induce apoptosis in vitro, and acetylate histone H4. While tenovin-1 demonstrates low genotoxicity, the compound has poor water solubility, which limits its uses in vivo.
| Molecular Weight | 369.48 |
| Formula | C20H23N3O2S |
| CAS Number | 380315-80-0 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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