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Z-VEID-FMK

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Catalog No.
A1923
Caspase-6抑制剂
组合的产品项目
规格价格库存 数量
1mg
¥ 1,100.00
现货
5mg
¥ 3,000.00
现货
10mg
¥ 5,000.00
现货
25mg
¥ 8,000.00
现货

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Background

When compared to other caspase inhibitors, Z-DRHD-FMK inhibited caspase 6 activity more effectively than the general caspase inhibitor Z-Val-Ala-Asp (OMe)-fluoromethy ketone (Z-VAD-FMK) or the caspase 6 inhibitor Z-Val-Glu(Ome)-Ile-Asp(OMe)-fluoromethyl ketone (Z-VEID-FMK). However, it was less effective in inhibiting TNFα-induced apoptosis than Z-VAD-FMK or Z-VEID-FMK, presumably because caspase 6 is only one of at least three effector caspases, the others being caspase 3 and 7, that are active during caspase dependent apoptosis. Loss of DNA-binding activity and TNFα-induced apoptosis can be prevented by caspase-6-preferred inhibitor (Z-VEID-FMK)1.

The caspase-6-specific inhibitor Z-VEID- FMK and general caspase inhibitors significantly prevent apoptosis of caspase-6-microinjected neurons2.

Z-VEID-FMK, which inhibits caspase-6, was also able to abolish the cleavage of procaspase-8, although caspase-6 is activated downstream of caspase-8 in Fas-mediated apoptosis3.

References:
1. Nyormoi et al (2003) Sequence-based discovery of a synthetic peptide inhibitor of caspase 6. Apoptosis 8 371.
2. Y. Zhang C. Goodyer, Selective and Protracted Apoptosis in Human Primary Neurons Microinjected with Active Caspase-3, -6, -7, and -8. The Journal of Neuroscience, 2000, 20(22):8384–8389
3. Microinjected with Active Caspase-3, -6, -7, and -8 Taimen and Kallajoki (2003) NuMA and nuclear lamins behave differently in Fas-mediated apoptosis. J.Cell Sci.116 571.

文献引用

1. Xie J, Guo H, et al. "Identification of cleavage of NS5A of C-strain classical swine fever virus." Arch Virol. 2016 Oct 20. PMID:27766426
2. Chen Y, Sun M, et al, "a novel PAC-1 derivative, activates procaspase-3 and causes cancer cell apoptosis." Cancer Chemother Pharmacol. 2016 Aug 3. PMID:27488460

Chemical Properties

StorageStore at -20°C
M.Wt652.71
FormulaC31H45FN4O10
SynonymsCaspase-6 inhibitor (fluoromethylketone),Benzyloxycarbonyl-Val-Glu(OMe)-Ile-​Asp(OMe)-fluoromethylketone
Solubility≥113.4mg/mL in DMSO
Chemical Namemethyl (4S)-5-[[(2S)-1-[[(3S)-5-fluoro-1-methoxy-1,4-dioxopentan-3-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-[[(2S)-3-methyl-2-(phenylmethoxycarbonylamino)butanoyl]amino]-5-oxopentanoate
SDFDownload SDF
Canonical SMILESCCC(C)C(C(=O)NC(CC(=O)OC)C(=O)CF)NC(=O)C(CCC(=O)OC)NC(=O)C(C(C)C)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

Cell experiment [1]:

细胞系

黄体细胞

制备方法

溶于DMSO。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

50 μM;6小时

实验结果

对于黄体细胞,与caspase-3,caspase-6和caspase-8抑制剂(分别为Z-DEVD-FMK,Z-VEID-FMK,Z-IETD-FMK)以及一般的caspase抑制剂(Boc-DFMK)一起孵育可以减少肿瘤坏死因子α诱导的DNA片段化。

References:

[1]. Abdo M1, Hisheh S, Dharmarajan A. Role of tumor necrosis factor-alpha and the modulating effect of the caspases in rat corpus luteum apoptosis. Biol Reprod. 2003 Apr;68(4):1241-8.

生物活性

Z-VEID-FMK是caspase-6/Mch2的特异性识别序列。
靶点 caspase-6          
IC50            

质量控制

化学结构

Z-VEID-FMK

相关生物数据

Z-VEID-FMK

相关生物数据

Z-VEID-FMK