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Z-VAD-FMK

Catalog No.
A1902
Pan-Caspase抑制剂。
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,500.00
现货
1mg
¥ 550.00
现货
5mg
¥ 1,500.00
现货
10mg
¥ 2,500.00
现货
25mg
¥ 4,000.00
现货

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Background

Z-VAD-FMK, an inhibitor of ICE-like proteases, inhibits apoptosis in THP.1 cells induced by diverse stimuli1 and Fas antigen-induced apoptosis in Jurkat T-cells2. It inhibits apoptosis by blocking the activation of proCPP32 into its active form, rather than by preventing the proteolytic action of CPP32 directly.

Z- VAD-FMK inhibits the formation of large kilobasepair fragments of DNA induced by diverse stimuli. Z-VAD-FMK had little or no effect on STS-induced necrotic cell death suggesting that the ICE-like protease activity was not involved in necrosis3.

Z-VAD-FMK almost completely inhibited the formation of large kilobasepair induced by all four stimuli. Similarly Z-VAD-FMK almost completely inhibited the enhanced formation of large kilobasepair fragments induced by thapsigargin or cycloheximide in the presence of TLCK, in good agreement with its ability to inhibit apoptosis induced by these treatments. These stimuli also induced internucleosomal cleavage of DNA, which was inhibited by Z-VAD-FMK. These results suggested that an ICE-like protease(s) acts at a stage prior to the formation of large kilobasepair fragments of DNA3.

References:
1. Darmon, A.J., Ehrman, N., Caputo, A., Fujinaga, J. and Bleackley, R.C. (1994) J. Biol. Chem. 269, 32043-32046.
2. Chow, S. C., Weis M., Kass, G. E. N., Holmstrom, T. H., Eriksson, J. E. and Orrenius S. (1995) FEBS Lett. 364, 134±138
3. H. Zhu et al./FEBS Letters 374 (1995) 303-308

文献引用

Chemical Properties

StorageStore at -20°C
M.Wt467.49
Cas No.187389-52-2
FormulaC22H30FN3O7
SynonymsBenzyloxycarbonyl-Val-Ala-Asp(OMe)-fluoromethylketone,Z-Val-Ala-Asp(OMe)-FMK
Solubility≥23.37mg/mL in DMSO
Chemical Namemethyl (3S)-5-fluoro-3-[[(2S)-2-[[(2S)-3-methyl-2-(phenylmethoxycarbonylamino)butanoyl]amino]propanoyl]amino]-4-oxopentanoate
SDFDownload SDF
Canonical SMILESCC(C)C(C(=O)NC(C)C(=O)NC(CC(=O)OC)C(=O)CF)NC(=O)OCC1=CC=CC=C1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

激酶实验[1]:

阻止CPP32加工成其活性形式

Z-VAD-FMK通过直接干扰CPP32的加工,抑制CPP32的激活,从而抑制细胞凋亡。

细胞实验[2]:

细胞系

人CD4+ (~ 97%)和CD8+ T (~ 98%)细胞

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应时间

24小时

应用

Z-VAD-FMK剂量依赖地抑制抗CD3和抗CD28共同刺激介导的T细胞增殖。Z-VAD-FMK在25和50 μM时效果较差,但在100 μM浓度时抑制T细胞增殖。

动物实验[3]:

动物模型

过敏性接触性皮炎(ACD)C57BL小鼠

剂量

1.25 mM

应用

1.25 mM Z-VAD-FMK处理组的小鼠其右耳廓肿胀程度,两只耳朵之间的重量差异和厚度均显著低于阴性对照组(NC)。而且,耳损伤部位INF-γ和IL-2的水平,T淋巴细胞内BrdU的平均强度以及活化标志物阳性的T淋巴细胞百分数也均比NC组更低。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Slee EA1, Zhu H, Chow SC 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]. Lawrence CP1, Chow SC. Suppression of human T cell proliferation by the caspase inhibitors, z-VAD-FMK and z-IETD-FMK is independent of their caspase inhibition properties. Toxicol Appl Pharmacol. 2012 Nov 15;265(1):103-12.

[3]. Li YY, Yan CL. Inhibition of elicitation of allergic contact dermatitis by topical use of Z-VAD-FMK, a broad caspase inhibitor: experiment in mice. Zhonghua Yi Xue Za Zhi. 2012 Jul 24;92(28):1992-6.

生物活性

Z-VAD-FMK是一种细胞通透性的,不可逆的广谱性Caspase抑制剂。在肿瘤细胞中,它可以抑制Caspase的加工和凋亡诱导,IC50为0.0015 - 5.8 mM。在体内也具有活性。
靶点 Caspase          
IC50 0.0015 - 5.8 mM          

质量控制

质量控制和MSDS

批次:

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