AGK7 是 Sirtuin 2 (SIRT2) 抑制剂。它在体外和帕金森病果蝇模型中均能抑制多巴胺能细胞的凋亡。在帕金森病细胞模型中,它改善了 α-突触核蛋白毒性和修饰的包涵体形态
产品描述
AGK7 is an inactive control of AGK2, a selective SIRT2 inhibitor that selectively inhibits SIRT3 over SIRT1 and SIRT2 (IC50 = >5 μM, >50 μM and >50 μM for SIRT3, SIRT1, and SIRT2, respectively).
体外活性
AGK2 is a selective SIRT2 inhibitor with IC50 value of 3.5 μM. AGK2 slightly inhibited SIRT1 and 3 only at concentrations over 40 μM. Relative to an inactive control AGK7, AGK2 increased acetylated tubulin. In H4 cells transfected with α-Syn, AGK2 reduced α-Syn-mediated toxicity in a dose-dependent way. By contrast, the inactive AGK7 had no effect. In H4 cells cotransfected withα-Syn and synphilin-1, the inactive AGK7 failed to affect a-Syn aggregation, whereas AGK2 promoted the formation of enlarged inclusions [1].
Cas No.
304896-21-7
分子式
C23H13Cl2N3O2
分子量
434.28
储存和溶解度
DMSO:0.5 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years