Tenovin-6 是 Tenovin-1 的类似物，能抑制二氢乳清酸脱氢酶。它也抑制纯化人 SIRT1、SIRT2 和 SIRT3 蛋白脱乙酰酶活性，IC50分别为 21 μM、10 μM 和 67 μM。它是一种p53转录活性的激活剂。

Tenovin-6 is a p53 transcriptional activity agonist.

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.

1011557-82-6

C25H34N4O2S

454.63

Tenovin 6

H2O:90 mg/mL (198 mM)
Ethanol:<1 mgml
DMSO:91 mg/mL (200.2 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years