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Z-IETD-FMK

现货
Catalog No.
B3232
Caspase-8抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 4,320.00
现货
20ul (10 mM)
¥ 1,250.00
现货
100ul (2 mM)
¥ 1,250.00
现货
1mg
¥ 1,400.00
现货
5mg
¥ 3,000.00
现货

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Background

Z-IETD-FMK is an inhibitor of caspase 8 [1].

Z-IETD-FMK inhibits T cell proliferation induced by PHA or anti-CD3 plus anti-CD28 without toxicity of resting T cells. The mechanism of this inhibition of Z-IETD-FMK has been proved not through the effect on IL-2 secretion or IFN-γ production but the decrease of CD25 expression. Experiments show that Z-IETD-FMK has no effect on normal cell growth when there is no activation signal. Z-IETD-FMK has also been found to significantly inhibit NF-κB activation when the concentration is 100μM [1].

Apart from the ability of inhibiting cell proliferation, Z-IETD-FMK is reported to inhibit TRAIL-mediated killing in cells. It protects the procaspases 9, 2, and 3, and protects PARP to a similar extent in both HCT116 and SW480 cells [2].

References:
[1] C.P. Lawrence, S.C. Chow. Suppression of human T cell proliferation by the caspase inhibitors, z-VAD-FMK and z-IETD-FMK is independent of their caspase inhibition properties. Toxicology and Applied Pharmacology. 2012, 265: 103-112.
[2] Nesrin Özören, Kunhong Kim, Timothy F. Burns, et al. The caspase 9 inhibitor Z-LEHD-FMK protects human liver cells while permitting death of cancer cells exposed to tumor necrosis factor-related apoptosis-inducing ligand. Cancer Research. 2000, 60: 6259-6265.

文献引用

Chemical Properties

StorageStore at -20°C
M.Wt654.68
Cas No.210344-98-2
FormulaC30H43FN4O11
SynonymsBenzyloxycarbonyl-Ile-Glu(OMe)-Thr-Asp(OMe)-fluoromethylketone, Z-Ile-Glu(OMe)-Thr-Asp(OMe)-FMK
Solubility≥32.734mg/mL in DMSO
Chemical Namemethyl 5-[[1-[(5-fluoro-1-methoxy-1,4-dioxopentan-3-yl)amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-[[3-methyl-2-(phenylmethoxycarbonylamino)pentanoyl]amino]-5-oxopentanoate
SDFDownload SDF
Canonical SMILESCCC(C)C(C(=O)NC(CCC(=O)OC)C(=O)NC(C(C)O)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

细胞实验: [1]

细胞系

纯化的CD4+和CD8+ T细胞

制备方法

溶解度有限,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

24 h

实验结果

使用[3H]-胸苷掺入测定T细胞增殖。z-IETD-FMK(100 μM)抑制T细胞增殖。在100 μM的z-IETD-FMK存在下,活化后约9%的对照活化T细胞摄取PI,细胞死亡增加至23%。此外,100 μM z-IETD-FMK降低活化T细胞中p65的核易位。

动物实验: [2]

动物模型

SHIP1-/- (CD45.1)小鼠

给药剂量

5 mg/kg,每周三次,持续3周

实验结果

与载体对照相比,Z-IETD-FMK处理的小鼠的小肠和肺中的解剖病理学显著减少。在Z-IETD-FMK处理的SHIP1-/-宿主的小肠和肺中CD3+T细胞数目显著恢复,而载体处理的SHIP1-/-宿主的T细胞缺乏。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

1. Lawrence CP, 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.

2. Park MY, Srivastava N, Sudan R et al. Impaired T-cell survival promotes mucosal inflammatory disease in SHIP1-deficient mice. Mucosal Immunol. 2014 Nov;7(6):1429-39.

生物活性

描述 Z-IETD-FMK是一种特异性的caspase 8抑制剂。
靶点 caspase 8          
IC50            

质量控制

化学结构

Z-IETD-FMK

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