AGK2 is a selective SIRT2 inhibitor with an IC50 of 3.5 μM. AGK2 inhibits SIRT1 and SIRT3 with IC50s of 30 and 91 μM, respectively.
IC50&Target
SIRT2
3.5 μM (IC50)
SIRT1
30 μM (IC50)
SIRT3
91 μM (IC50)
体外研究
AGK2 significantly inhibits cell proliferation in a dose-dependent manner. AGK2 also significantly inhibits cell growth in a dose-dependent manner without inducing cytotoxicity at low doses. Twelve days after AGK2 (5 μM) treatment, cells show a significantly reducing colony forming ability in soft agar to 46% of the control cells. Western blot analysis shows that the levels of CDK4 or CDK6 and cyclin D1 are decreased after AGK2 treatment in a dose-dependent manner. In addition, AGK2 inhibits the expression of p53 protein. Treatment of microglial BV2 cells with 10 μM AGK2 leads to a significant increase in PAR signals. Treatment of microglial BV2 cells with 10 μM AGK2 also leads to a significant decrease in the intracellular ATP and significant increases in both late-stage apoptosis and necrosis of the cells.
体内研究
AGK2 significantly reduces mortality and decreases levels of cytokines in blood (TNF-α: 298.3±24.6 vs 26.8±2.8 pg/mL, p=0.0034; IL-6: 633.4±82.8 vs 232.6±133.0 pg/mL, p=0.0344) and peritoneal fluid (IL-6: 704.8±67.7 vs 391.4±98.5 pg/mL, p=0.033) compare to vehicle control. AGK2 also suppresses the TNF-α and IL-6 production in the culturing splenocytes (TNF-α: 68.1±6.4 vs 23.9±2.8 pg/mL, p=0.0009; IL-6: 73.1±4.2 vs 49.6±3.0 pg/mL; p=0.0051).
分子式
C23H13N3O2Cl2
分子量
434.27
CAS号
304896-28-4
运输条件
Room temperature in continental US; may vary elsewhere.