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Z-IETD-FMK

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Chemical Structure| 210344-98-2 同义名 : Z-IE(OMe)TD(OMe)-FMK;Caspase-8 Inhibitor;Z-Ile-Glu(OMe)-Thr-Asp(OMe)-CH₂F.;MDK4982;Granzyme B Inhibitor III
CAS号 : 210344-98-2
货号 : A772438
分子式 : C30H43FN4O11
纯度 : 98%+
分子量 : 654.681
MDL号 : MFCD03490491
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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：
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]
实验方案
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
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.