Z-IETD-FMK,英文名:Z-IETD-FMK,CAS:210344-98-2,化学式:C30H43FN4O11,分子量:654.68,密度:1.247±0.06 g/cm3(Predicted)
210344-98-2
Z-IETD-FMK(Z-IETD-FMK)
CAS: 210344-98-2
化学式: C30H43FN4O11
| 中文名 | Z-IETD-FMK |
| 英文名 | Z-IETD-FMK |
| 别名 | 化合物Z-IETD-FMK (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 |
| 英文别名 | Z-IETD-FMK GRANZYME B INHIBITOR III Z-ILE-GLU(OME)-THR-ASP(OME)-FMK Z-ILE-GLU(OME)-THR-ASP(OME)-FLUOROMETHYLKETONE Z-ILE-GLU(OME)-THR-DL-ASP(OME)-FLUOROMETHYLKETONE BENZYLOXYCARBONYL-ILE-GLU(OME)-THR-ASP(OME)-FLUOROMETHYLKETONE |
| CAS | 210344-98-2 |
| 化学式 | C30H43FN4O11 |
| 分子量 | 654.68 |
| 密度 | 1.247±0.06 g/cm3(Predicted) |
| 沸点 | 925.7±65.0 °C(Predicted) |
| 溶解度 | 溶于DMSO |
| 酸度系数 | 11.12±0.46(Predicted) |
| 存储条件 | under inert gas (nitrogen or Argon) at 2-8°C |
| 体外研究 | 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. |
| 体内研究 | 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. |
210344-98-2 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.527 ml | 7.637 ml | 15.275 ml |
| 5 mM | 0.305 ml | 1.527 ml | 3.055 ml |
| 10 mM | 0.153 ml | 0.764 ml | 1.527 ml |
| 5 mM | 0.031 ml | 0.153 ml | 0.305 ml |
210344-98-2 - 简介
Z-IETD-FMK是一种化合物，全名为N-benzyloxycarbonyl-Ile-Glu (O-methyl)-Thr-Asp- [fmoc- Lys(Dabcyl)]-N-(4-methylcarbamate)。它是一种特定类型的肽酶抑制剂。Z-IETD-FMK主要用作刺激性细胞因子介导的凋亡（细胞死亡）的细胞信号转导途径的研究工具。它可以选择性地抑制半胱天冬氨酸蛋白酶（caspase）-8的活性，从而阻断凋亡信号传递。
制备Z-IETD-FMK的方法一般涉及多步合成化学反应。通常是通过化学合成将相应的氨基酸和它们的侧链保护基逐步构建起来，最后与其他功能性基团反应生成Z-IETD-FMK。
这是一种化学品，具有潜在的危险性。应该严格按照化学实验室的安全操作程序来处理和储存该化合物。对于无经验或未受过专业培训的人员，不推荐在家庭或非实验室环境中使用。使用时，应佩戴个人防护装备，包括实验室手套，眼镜和实验室外套，以避免皮肤接触和吸入。不要吞食或吸入Z-IETD-FMK，并远离儿童和宠物。最后更新：2024-04-09 19:05:17
