Z-VAD-FMK
Catalog No.
A1902
Pan-Caspase抑制剂。
Featured Products
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Z-VAD-FMK是ICE-样蛋白酶（Caspase）的抑制剂。在THP.1细胞中，Z-VAD-FMK可以抑制不同刺激诱导的凋亡。在Jurkat T细胞中，它可以抑制Fas抗原诱导的凋亡。Z-VAD-FMK通过阻断proCPP32活化，而非阻止CPP32的蛋白水解活性从而抑制细胞凋亡。
Z-VAD-FMK抑制不同刺激诱导下的大的DNA片段的形成，且几乎可以完全抑制所有四个刺激诱导下的大的DNA片段的形成。在TLCK存在时，Z-VAD-FMK也可以完全抑制由thapsigargin或cycloheximide诱导的大DNA片段的增加，这与Z-VAD-FMK能够抑制这些处理诱导的凋亡是一致的。这些结果表明Caspase作用于大的DNA片段形成之前的阶段。
Z-VAD-FMK对STS诱导的细胞坏死几乎没有效果，表明Caspase不参与细胞坏死的发生[3]。
参考文献：
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| Storage | Store at -20°C |
| M.Wt | 467.49 |
| Cas No. | 187389-52-2 |
| Formula | C22H30FN3O7 |
| Synonyms | Benzyloxycarbonyl-Val-Ala-Asp(OMe)-fluoromethylketone,Z-Val-Ala-Asp(OMe)-FMK |
| Solubility | ≥23.37 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | methyl (3S)-5-fluoro-3-[[(2S)-2-[[(2S)-3-methyl-2-(phenylmethoxycarbonylamino)butanoyl]amino]propanoyl]amino]-4-oxopentanoate |
| SDF | Download SDF |
| Canonical SMILES | CC(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 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。溶液形式一般不宜长期储存，请尽快用完。 |
| 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°C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°C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. |
|
| 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 | |||||
质量控制和MSDS
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