货号:A772438 同义名: Z-IE(OMe)TD(OMe)-FMK;Caspase-8 Inhibitor
Z-IETD-FMK is a specific Caspase-8 inhibitor.
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产品名称 | Capase-7 ↓ ↑ | Caspase ↓ ↑ | Caspase-1 ↓ ↑ | Caspase-10 ↓ ↑ | Caspase-2 ↓ ↑ | Caspase-3 ↓ ↑ | Caspase-4 ↓ ↑ | Caspase-5 ↓ ↑ | Caspase-6 ↓ ↑ | Caspase-8 ↓ ↑ | Caspase-9 ↓ ↑ | 其他靶点 | 纯度 | ||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Emricasan | ✔ | 99%+ | |||||||||||||||||
Z-VAD(OMe)-FMK | ✔ | 99%+ | |||||||||||||||||
Z-VAD-FMK | ✔ | 99%+ | |||||||||||||||||
Q-VD-OPh | 97% | ||||||||||||||||||
VX-765 |
++++
Caspase-1, Ki: 0.8 nM |
++++
Caspase-4, Ki: <0.6 nM |
99%+ | ||||||||||||||||
Ac-DEVD-CHO |
+++
caspase-7, Ki: 1.6 nM |
+++
Caspase-1, Ki: 18 nM |
+++
caspase-10, Ki: 12 nM |
+
caspase-2, Ki: 1.71 μM |
++++
Caspase-3, Ki: 230 pM |
++
Caspase-4, Ki: 132 nM |
++
caspase-5, Ki: 205 nM |
+++
caspase-6, Ki: 31 nM |
++++
caspase-8, Ki: 0.92 nM |
++
Caspase-9, Ki: 60 nM |
98%+ | ||||||||
Z-DEVD-FMK | ✔ | 98% | |||||||||||||||||
Z-IETD-FMK | ✔ | 98%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Caspase-8, belong to the Caspase family, is a cysteine protease which plays a key role in the initiation of apoptotic signaling pathway via death receptors. Z-IETD-FMK is a specific Caspase-8 inhibitor. Incubation with 20μM Z-IETD-FMK can inhibited the hsp27-comsuption-induced 30- and 20-kDa cleavage of Caspase-8, as well as showed partial inactivation of Caspase-3, in lysates of retinal cells, suggesting the selective inhibition of Caspase-8 by Z-IETD-FMK. Also, treatment with Z-IETD-FMK only dose-dependently decreased stress-induced caspase-3–like activity by incubation with hsp27 antibody, but not ischemia, AMPA or NMDA, in retinal cells[1]. For Caspase-8 also a critical role during protozoan infection, blockade of caspase-8 by treatment with Z-IETD-FMK disturbed IL-2 production and induction of NF- B responses to TCR:CD3 engagement in T cell cultures. Injection of 0.4mg Z-IETD-FMK increased susceptibility to protozoan parasite Trypanosoma cruzi. infection in mice[2]. |
作用机制 | Z-IETD-FMK is the substrate for caspase, which can bind to the active site to form an irreversible bond with the enzyme thus blocking it from further action.[3] |
Dose | Mice: 10 mg/kg (co with doxorubicin)[4] |
Administration | i.p. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.53mL 0.31mL 0.15mL |
7.64mL 1.53mL 0.76mL |
15.27mL 3.05mL 1.53mL |
CAS号 | 210344-98-2 |
分子式 | C30H43FN4O11 |
分子量 | 654.681 |
别名 | Z-IE(OMe)TD(OMe)-FMK;Caspase-8 Inhibitor;Z-Ile-Glu(OMe)-Thr-Asp(OMe)-CH₂F.;MDK4982;Granzyme B Inhibitor III |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,2-8°C |
溶解度 |
DMSO: 40 mg/mL(61.1 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 |
动物实验配方 |