货号:Z5936
储存条件:粉末-20°C可保存3年;液体-80°C可保存12月。
产品描述
ICE (Interleukin-1βconverting enzyme)-like proteases, play a key role in the Fas-induced apoptosis in thymocytes. Z-VAD(OMe)-FMK, also called as Z-VAD-FMK, is ICE-like protease (Caspase-1, Caspase-3, Caspase-4, Caspase-5, Caspase-2, Caspase-6 and Caspase-7) inhibitor. Treatment with Z-VAD(OMe)-FMK at concentration of 10μM for 4h caused inhibition of caspase-3 cleavage at both these junctions to yield the p17 subunit in THP.1 cells exposed to an apoptotic stimulus TLCK. This cleavage could be also observed in Jurkat cells induced to undergo apoptosis by Fas antibody. These indicated that Z-VAD(OMe)-FMK could block the processing of CPP32. However, Z-VAD(OMe)-FMK did not inhibit the proteolysis of PARP, an early biochemical marker of apoptosis and also the substrate of ICE-like proteases, in cell lysates. These suggested that Z-VAD(OMe)-FMK did not inhibit CPP32 activity directly, but may block apoptosis by inhibiting the processing of CPP32. Subcutaneous administration of Z-VAD(OMe)-FMK at dose of 10mg/kg caused total lung neutrophil count increase due to inhibiting neutrophil apoptosis by Z-VAD(OMe)-FMK, as well as increase of lung cytokine response in PVM (pneumovirus pneumonia virus)-infected mice without decreasing lung caspase-3 activity directly.
作用机制
Z-VAD(OMe)-FMK can inhibit Fas-induced apoptosis by preventing the activation of proCPP32 (pro-Caspase-3) into its active form, rather than by blocking the proteolytic action of CPP32 (Caspase-3) directly.
储存液制备 | 质量 | 1 mg | 5 mg | 10 mg |
1 mM | 2.1391 mL | 10.6954 mL | 21.3908 mL | |
5 mM | 0.4278 mL | 2.1391 mL | 4.2782 mL | |
10 mM | 0.2139 mL | 1.0695 mL | 2.1391 mL |
产品性质
CAS号 | 187389-52-2 | ||
分子式 | C22H30FN3O7 | ||
分子量 | 467.49 | ||
溶解度 | DMSO | 500.0 mg/mL (1069.5 mM) warming | |
Water | lnsoluble | ||
动物实验配方 | IP | 2% DMSO+2% Tween80+40% PEG300+water | 10 mg/mL,clear |
PO | 0.5% CMC-Na | 25 mg/mL,suspension |