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Z-VAD(OMe)-FMK {[allProObj[0].p_purity_real_show]}

货号:A354225 同义名: Z-Val-Ala-Asp(OMe)-FMK;Z-Val-Ala-Asp-(OMe)-Fluoromethyl Ketone

Z-VAD(OMe)-FMK是一种细胞可透性、不可逆的广谱caspase抑制剂,可阻止所有形式的细胞凋亡。

Z-VAD(OMe)-FMK 化学结构 CAS号:187389-52-2
Z-VAD(OMe)-FMK 化学结构
CAS号:187389-52-2
Z-VAD(OMe)-FMK 3D分子结构
CAS号:187389-52-2
Z-VAD(OMe)-FMK 化学结构 CAS号:187389-52-2
Z-VAD(OMe)-FMK 3D分子结构 CAS号:187389-52-2
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Z-VAD(OMe)-FMK 纯度/质量文件 产品仅供科研

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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-VAD(OMe)-FMK 生物活性

靶点
  • Caspase

描述 ICE (Interleukin-1βconverting enzyme)-like proteases, play a key role in the Fas-induced apoptosis in thymocytes. Z-VAD(OMe)-FMK, also called as Z-VAD-FMK, is ICE-like protease (Caspase-1, Caspase-3, Caspase-4, Caspase-5, Caspase-2, Caspase-6 and Caspase-7) inhibitor. Treatment with Z-VAD(OMe)-FMK at concentration of 10μM for 4h caused inhibition of caspase-3 cleavage at both these junctions to yield the p17 subunit in THP.1 cells exposed to an apoptotic stimulus TLCK. This cleavage could be also observed in Jurkat cells induced to undergo apoptosis by Fas antibody. These indicated that Z-VAD(OMe)-FMK could block the processing of CPP32. However, Z-VAD(OMe)-FMK did not inhibit the proteolysis of PARP, an early biochemical marker of apoptosis and also the substrate of ICE-like proteases, in cell lysates. These suggested that Z-VAD(OMe)-FMK did not inhibit CPP32 activity directly, but may block apoptosis by inhibiting the processing of CPP32[1]. Subcutaneous administration of Z-VAD(OMe)-FMK at dose of 10mg/kg caused total lung neutrophil count increase due to inhibiting neutrophil apoptosis by Z-VAD(OMe)-FMK, as well as increase of lung cytokine response in PVM (pneumovirus pneumonia virus)-infected mice without decreasing lung caspase-3 activity directly[2].
作用机制 Z-VAD(OMe)-FMK can inhibit Fas-induced apoptosis by preventing the activation of proCPP32 (pro-Caspase-3) into its active form, rather than by blocking the proteolytic action of CPP32 (Caspase-3) directly.[1]

Z-VAD(OMe)-FMK 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
3T9 MEFs Function Assay 16h increases cytochrome c release after etoposide-treatment 22613767
3T9 MEFs Function Assay 18h upregulates initiator caspase-9 but downregulates effector caspases after etoposide treatment 22613767
4T1 2.5-10μM Cell Viability Assay 4h rescues the cytotoxicity of 4T1 cells induced by SPDT in a concentration dependent manner 24206161
5637 20μM Apoptosis Assay 1h reverses CM-induced cell death 24282433

Z-VAD(OMe)-FMK 动物研究

Dose Rat: 3 mg/kg[3] (i.v.) Mice: 2 mg/kg - 10 mg/kg[2] (intranasal instillation)
Administration i.v., intranasal instillation

Z-VAD(OMe)-FMK 参考文献

[1]Slee EA, Zhu H, et al. Benzyloxycarbonyl-Val-Ala-Asp (OMe) fluoromethylketone (Z-VAD.FMK) inhibits apoptosis by blocking the processing of CPP32. Biochem J. 1996 Apr 1;315 ( Pt 1):21-4.

[2]van den Berg E, Bal SM, et al. The caspase inhibitor zVAD increases lung inflammation in pneumovirus infection in mice. Physiol Rep. 2015 Mar;3(3). pii: e12332.

Z-VAD(OMe)-FMK 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.70mL

2.14mL

1.07mL

21.39mL

4.28mL

2.14mL

Z-VAD(OMe)-FMK 技术信息

CAS号187389-52-2
分子式C22H30FN3O7
分子量 467.488
别名 Z-Val-Ala-Asp(OMe)-FMK;Z-Val-Ala-Asp-(OMe)-Fluoromethyl Ketone;Z-VAD-FMK
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(224.6 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

IP 2% DMSO+2% Tween80+40% PEG300+water 10 mg/mL clear

PO 0.5% CMC-Na 25 mg/mL suspension

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