AGK2

Research use only, not for human use.

AGK2（IC50=3.5 μM） is an effective, and specific SIRT2 inhibitor.

AGK-2 is a potent and selective inhibitor of sirtuin 2 (SIRT2).

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.

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).

AGK-2 | AGK-2 | AGK-2

Angiogenesis

PDE

SIRT2

Cancer

——

304896-28-4

434.27

C23H13Cl2N3O2

>98% (HPLC)

DMSO : 6 mg/mL 13.82 mM

c1cc2c(cccn2)c(c1)NC(=O)/C(=C/c1ccc(o1)c1c(ccc(c1)Cl)Cl)/C#N

2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide

(-20℃)

With Ice Pack

≥ 2 years