GlpBio

Boc-D-FMK

目录号: GC16774纯度: >95.00%同义词: (3S)-3-[[叔丁氧羰基]氨基]-5-氟-4-氧代-戊酸甲酯,Caspase Inhibitor III, Boc-Asp(OMe)-FMK, Boc-D(OMe)-FMK, Caspase3-Inhibitor BOC-D-FMK, Boc-Asp(OMe)-fluoromethylketone

Boc-D-FMK is a cell-permeable broad-spectrum caspase inhibitor that fully inhibits the pro-apoptotic effect of tumor necrosis factor-α (TNFα) with the half maximal inhibition concentration IC50 value of 39 μM .

Boc-D-FMK
Cas No.: 634911-80-1
规格价格库存数量操作
1mg¥350.00现货
1
5mg¥875.00现货
1
10mg¥1,400.00现货
1
25mg¥2,590.00现货
1
50mg¥3,780.00现货
1
10mM (in 1mL DMSO)¥1,014.00现货
1
电话: 400-920-5774Email: sales@glpbio.cn

文献被引

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产品描述 Description

Boc-D-FMK is a cell-permeable broad-spectrum caspase inhibitor that fully inhibits the pro-apoptotic effect of tumor necrosis factor-α (TNFα) with the half maximal inhibition concentration IC50 value of 39 μM [1].

Boc-D-FMK has been found to reduce the activation of nuclear factor kappa light chain enhancer of activated B cells (NF-kB), suppress the phosphorylation of subunit nuclear factor kappa light polypeptide gene enhancer in B cells inhibitor α (IkBα) and inhibits TNF-induced expression of intercellular adhesion molecule 1 (ICAM-1) and vascular cell adhesion molecule 1 (VCAM-1) [2].

Moreover, Boc-D-FMK has also effectively attenuated the hepatocyte apoptosis in bile duct-ligated rats potentially improving the survival rates [3].

References:
[1] Cowburn AS, White JF, Deighton J, Walmsley SR, Chilvers ER. z-VAD-fmk augmentation of TNF alpha-stimulated neutrophil apoptosis is compound specific and does not involve the generation of reactive oxygen species. Blood. 2005 Apr 1;105(7):2970-2. Epub 2004 Nov 30.
[2] Wu X, Guo R, Chen P, Wang Q, Cunningham PN. TNF induces caspase-dependent inflammation in renal endothelial cells through a Rho- and myosin light chain kinase-dependent mechanism. Am J Physiol Renal Physiol. 2009 Aug;297(2):F316-26. doi: 10.1152/ajprenal.00089.2009. Epub 2009 May 6.
[3] Sheen-Chen SM, Hung KS, Eng HL. Effect of Boc-D-Fmk on hepatocyte apoptosis after bile duct ligation in rat and survival rate after endotoxin challenge. J Gastroenterol Hepatol. 2008 Aug;23(8 Pt 1):1276-9. doi: 10.1111/j.1440-1746.2008.05368.x. Epub 2008 Mar 27.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

C57BL/6 mice renal endothelial cells

Preparation method

The solubility of this compound in DMSO is >11.65 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

100 μM for 3 h

Applications

Renal EC apoptosis after 4 h of TNF exposure was strongly inhibited by pretreatment with the broad-spectrum caspase inhibitor Boc-D-fmk, as well as caspase-3 inhibitor z-DQMD-fmk. Pretreatment with broad-spectrum caspase inhibitor Boc-D-fmk significantly inhibited TNF-induced ICAM-1 and VCAM-1 mRNA expression.
Animal experiment [2]:

Animal models

Male Sprague–Dawley rats

Dosage form

1.5 mg/kg, i.p.

Application

When compared with sham operation, common bile duct ligation with ZFA-fmk (placebo) significantly increased hepatocyte apoptosis. When compared with the OBZFA group, Boc-D-FMK significantly diminished the increased hepatocyte apoptosis in the OBBOC-D group. There is no difference in hepatocyte apoptosis between OBBOC-D and SHAM groups. After endotoxin challenge, the 48 h survival rates were 100%, 87.5% and 62.5% for the SHAM, OBBOC-D and OBZFA groups, respectively。

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Wu X, Guo R, Chen P, Wang Q, Cunningham PN. TNF induces caspase-dependent inflammation in renal endothelial cells through a Rho- and myosin light chain kinase-dependent mechanism. Am J Physiol Renal Physiol. 2009 Aug;297(2):F316-26. doi: 10.1152/ajprenal.00089.2009. Epub 2009 May 6.

[2] Sheen-Chen SM, Hung KS, Eng HL. Effect of Boc-D-Fmk on hepatocyte apoptosis after bile duct ligation in rat and survival rate after endotoxin challenge. J Gastroenterol Hepatol. 2008 Aug;23(8 Pt 1):1276-9. doi: 10.1111/j.1440-1746.2008.05368.x. Epub 2008 Mar 27.

产品文档 Product Documents

Purity:>95.00%

化学性质Chemical Properties

CAS 号
634911-80-1
同义词
(3S)-3-[[叔丁氧羰基]氨基]-5-氟-4-氧代-戊酸甲酯,Caspase Inhibitor III, Boc-Asp(OMe)-FMK, Boc-D(OMe)-FMK, Caspase3-Inhibitor BOC-D-FMK, Boc-Asp(OMe)-fluoromethylketone
化学名
methyl 5-fluoro-3-[(2-methylpropan-2-yl)oxycarbonylamino]-4-oxopentanoate
SMILES
CC(C)(C)OC(=O)NC(CC(=O)OC)C(=O)CF
分子式
C11H18FNO5
分子量
263.26 g/mol
溶解性
≥ 11.65mg/mL in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol