CASPASE-8抑制剂
中文名称 | CASPASE-8抑制剂 |
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中文同义词 | (5S,8S,11S,14S)-5-((S)-仲丁基)-14-(2-氟乙酰基)-11-((R)-1-羟乙基)-8-(3-甲氧基-3-氧代丙基)-3,6,9,12-四氧代-1-苯基-2-氧杂-4,7,10,13-四氮杂十六烷-16-酸甲酯;CASPASE-8抑制剂;化合物Z-IETD-FMK |
英文名称 | CASPASE-8 INHIBITOR II |
英文同义词 | BENZYLOXYCARBONYL-ILE-GLU(OME)-THR-ASP(OME)-FLUOROMETHYLKETONE;GRANZYME B INHIBITOR III;CASPASE-8 INHIBITOR II;CASPASE-3 PROCESSING ENZYME INHIBITOR (FLUOROMETHYLKETONE);Z-ILE-GLU(OME)-THR-ASP(OME)-FLUOROMETHYLKETONE;Z-ILE-GLU(OME)-THR-ASP(OME)-FMK;Z-ILE-GLU(OME)-THR-DL-ASP(OME)-FLUOROMETHYLKETONE;Z-IE(OME)TD(OME)-FLUOROMETHYLKETONE |
CAS号 | 210344-98-2 |
分子式 | C30H43FN4O11 |
分子量 | 654.68 |
EINECS号 | |
相关类别 | Caspases/Apoptosis;Caspase/Related Products |
Mol文件 | Mol File |
结构式 |
CASPASE-8抑制剂 性质
沸点 | 925.7±65.0 °C(Predicted) |
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密度 | 1.247±0.06 g/cm3(Predicted) |
储存条件 | under inert gas (nitrogen or Argon) at 2-8°C |
溶解度 | 溶于二甲基亚砜 |
形态 | 粉末 |
酸度系数(pKa) | 11.12±0.46(Predicted) |
颜色 | 白色至浅黄色 |
Target | Value |
Caspase-8 |
Z-IETD-FMK causes full inhibition only of the proapoptotic effect of TNFα with an IC 50 of 0.46 μM. Z-IETD-FMK and Z-VAD-FMK at non-toxic doses are found to be immunosuppressive and inhibit human T cell proliferation induced by mitogens and IL-2. They are shown to block NF-κB in activated primary T cells, but have little inhibitory effect on the secretion of IL-2 and IFN-γ during T cell activation. Z-IETD-FMK inhibits the cleavage of caspase-8 and only partially inhibits the cleavage of caspase-3 and PARP. Z-IETD-FMK can prevent the execution of apoptosis in retinal cells exposed to different apoptotic stimuli.
Pharmacological inhibition of caspase-8 by z-IETD-FMK robustly reduces tumour outgrowth and this is closely associated with a reduction in the release of pro-inflammatory cytokines, IL-6, TNF-α, IL-18, IL-1α, IL-33, but not IL-1β. Furthermore, inhibition of caspase-8 reduces the recruitment of innate suppressive cells, such as myeloid-derived suppressor cells, but not of regulatory T cells to lungs of tumour-bearing mice.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/08/19 | S7314 | CASPASE-8抑制剂 Z-IETD-FMK | 210344-98-2 | 1mg | 1624.01元 |
2024/08/19 | S7314 | CASPASE-8抑制剂 Z-IETD-FMK | 210344-98-2 | 5mg | 4832.1元 |