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Z-IETD-FMK {[allProObj[0].p_purity_real_show]}

货号:A772438 同义名: Z-IE(OMe)TD(OMe)-FMK;Caspase-8 Inhibitor

Z-IETD-FMK is a specific Caspase-8 inhibitor.

Z-IETD-FMK 化学结构 CAS号:210344-98-2
Z-IETD-FMK 化学结构
CAS号:210344-98-2
Z-IETD-FMK 3D分子结构
CAS号:210344-98-2
Z-IETD-FMK 化学结构 CAS号:210344-98-2
Z-IETD-FMK 3D分子结构 CAS号:210344-98-2
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Z-IETD-FMK 纯度/质量文件 产品仅供科研

货号:A772438 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

Z-IETD-FMK 生物活性

靶点
  • Caspase-8

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]

Z-IETD-FMK 动物研究

Dose Mice: 10 mg/kg (co with doxorubicin)[4]
Administration i.p.

Z-IETD-FMK 参考文献

[1]Tezel G, Wax MB, et al. Inhibition of caspase activity in retinal cell apoptosis induced by various stimuli in vitro. Invest Ophthalmol Vis Sci. 1999 Oct;40(11):2660-7.

[2]Silva EM, Guillermo LV, et al. Caspase-8 activity prevents type 2 cytokine responses and is required for protective T cell-mediated immunity against Trypanosoma cruzi infection. J Immunol. 2005 May 15;174(10):6314-21.

[3]Taimen P, Kallajoki M, et al. NuMA and nuclear lamins behave differently in Fas-mediated apoptosis. J Cell Sci. 2003 Feb 1;116(Pt 3):571-83.

[4]Shi J, Zhang L, et al. Downregulation of doxorubicin-induced myocardial apoptosis accompanies postnatal heart maturation. Am J Physiol Heart Circ Physiol. 2012;302(8):H1603-13.

Z-IETD-FMK 实验方案

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

Z-IETD-FMK 技术信息

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
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