ApexBio/Boc-D-FMK/10mM(在1mL二甲基亚砜中)/A1904

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¥10000.00
货号:A1904
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Boc-D-FMKPan-caspase inhibitor

Catalog No.A1904
SizePriceStockQty
10mM (in 1mL DMSO)
$145.00
In stock
1mg
$50.00
In stock
5mg
$150.00
In stock
10mg
$225.00
In stock
25mg
$500.00
In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Sandlin RD, Wong KHK, et al. "Preservative solution that stabilizes erythrocyte morphology and leukocyte viability under ambient conditions." Sci Rep.2017 Jul 18;7(1):5658.PMID:28720788

Related Compound Libraries

  • DiscoveryProbe™ Bioactive Compound Library
  • DiscoveryProbe™ Apoptosis Compound Library

Quality Control

Quality Control & MSDS

View current batch:
    Purity = 98.00%
  • COA (Certificate Of Analysis)
  • NMR (Nuclear Magnetic Resonance)
  • MSDS (Material Safety Data Sheet)
  • Datasheet

Chemical structure

Boc-D-FMK

Related Biological Data

Boc-D-FMK

Biological Activity

DescriptionBOC-D-FMK is a Novel inhibitor of Caspase-3.
TargetsCaspase
IC50

Protocol

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.

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Chemical Properties

Cas No. 187389-53-3,634911-80-1SDF Download SDF
Synonyms Caspase Inhibitor III, Boc-Asp(OMe)-FMK, Boc-D(OMe)-FMK, Caspase3-Inhibitor BOC-D-FMK, Boc-Asp(OMe)-fluoromethylketone
Chemical Name methyl 5-fluoro-3-[(2-methylpropan-2-yl)oxycarbonylamino]-4-oxopentanoate
Canonical SMILES CC(C)(C)OC(=O)NC(CC(=O)OC)C(=O)CF
Formula C11H18FNO5 M.Wt 263.26
Solubility ≥11.65mg/mL in DMSO Storage Store at -20°C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Research Update

1. 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. Epub2008 Mar 27.Abstract Boc-D-FMK, a caspase inhibitor, was evaluated for its effect on hepatocyte apoptosis and on survival rate after bile duct ligation in rats.

Background

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.

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