Tenovin-6 is a p53 transcriptional activity agonist.

SIRT2:10 μM, SIRT3:67 μM, SIRT1:21 μM

Tenovins are active on mammalian cells at one-digit micromolar concentrations and decrease tumor growth in vivo as single agents. Tenovin-6 (50 mg/kg, i.p.) inhibits the growth of tumor in mice[1].

Assays are carried out using purified components in the Fluor de Lys Fluorescent Assay Systems. Relevant FdL substrates are used at 7 μM and NAD+ at 1 mM. Tenovins are solubilized in DMSO with the final DSMO concentration in the reaction being less than 0.25%. For SirT1 and HDAC8, one unit of enzyme is used per reaction, and for SirT2 and SirT3, five units is used per reaction. Reactions are carried out at 37°C for 1 hr.

The MTS assay is used to evaluate cell viability. UM cells are seeded into each well of 96-well plates (5,000 cells/well) and treated the next day with control or Tenovin-6 in an increasing concentrations from 0 to 20?μM for 68?h, and then MTS is added at 20?μL/well to be read at a wave length of 490?nm, the IC50 is determined by curve fitting of the sigmoidal dose-response curve.