Z-VAD(OMe)-FMK
产品说明书
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同义名 : | Z-Val-Ala-Asp(OMe)-FMK;Z-Val-Ala-Asp-(OMe)-Fluoromethyl Ketone;Z-VAD-FMK |
| CAS号 : | 187389-52-2 | |
| 货号 : | A354225 | |
| 分子式 : | C22H30FN3O7 | |
| 纯度 : | 99%+ | |
| 分子量 : | 467.488 | |
| MDL号 : | MFCD02684037 | |
| 存储条件： |
Pure form Inert atmosphere,Store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(224.6 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 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 |
| 生物活性 | |||
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| 靶点 |
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| 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[1]. 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[2]. | ||
| 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.[1] |
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| 细胞研究 | |||||
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| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
| 3T9 MEFs | Function Assay | 16h | increases cytochrome c release after etoposide-treatment | 22613767 | |
| 3T9 MEFs | Function Assay | 18h | upregulates initiator caspase-9 but downregulates effector caspases after etoposide treatment | 22613767 | |
| 4T1 | 2.5-10μM | Cell Viability Assay | 4h | rescues the cytotoxicity of 4T1 cells induced by SPDT in a concentration dependent manner | 24206161 |
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.14mL 0.43mL 0.21mL |
10.70mL 2.14mL 1.07mL |
21.39mL 4.28mL 2.14mL |
| 参考文献 |
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