Pitstop2 是一种选择性的两性蛋白结合的网格蛋白末端结构域抑制剂,IC50 值为 12 μM。 Pitstop2 严重干扰受体介导的内吞作用、HIV 进入和突触小泡循环。
产品描述
Pitstop2 is a selective inhibitor of amphiphysin association of clathrin terminal domain with an IC50 value of 12 μM. Pitstop2 acutely interferes with receptor-mediated endocytosis, entry of HIV, and synaptic vesicle recycling.
体外活性
Pitstop2 potently and specifically reduced HIV-1 infectivity by >90% in HeLa cells. Preincubation of HeLa cells with Pitstop2 (Pitstops 2) leads to a dose-dependent inhibition of Tf uptake with an IC50 value (12-5 μM). Application of 30 μM Pitstop2 completely blocked Tf endocytosis. Pitstop2-induced block of Tf endocytosis in HeLa cells was completely reversed within 1-3 hr of drug washout. In U2OS cells, the IC50 for Tf uptake is 9.7 μM. Pitstop 2 also causes a potent inhibition of EGF uptake[1].
Cas No.
1419320-73-2
分子式
C20H13BrN2O3S2
分子量
473.36
别名
Pitstop 2
储存和溶解度
DMSO:62.5 mg/mL (132.03 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years