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  • 产品名称：Z-WEHD-FMK(Caspase-1,4,5Inhibitor)

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  • 产品厂商：KamiyaBiomedical
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简单介绍：
Z-WEHD-FMK(Caspase-1,4,5Inhibitor)
详情介绍：
Purpose Irreversible caspase-1, 4, 5 inhibitor 
Sequence Z-Trp-Glu(OMe)-His-Asp(OMe)-CH2F (TFA salt), Z-WEHD-FMK
Specificity Inhibitor of Caspase-1/ICE, Caspase-4, and Caspase-5. Very weak inhibition of Caspase-9. No inhibition of Caspases-2 or -6.
Characteristics Trifluoroacetic acid salt of the fluoromethyl ketone peptide inhibitor of Caspases-1/ICE, -4, and -5.
The CH2F (fluoromethyl ketone) inhibitor has several advantages over other types of derivatives: Penetrates cell membranes, Not toxic to cells, Irreversible inhibition
Caspase-1 (also known as ICE), Caspase-4 (also known as ICErel-II, TX, or ICH-2), and Caspase-5 (also known as ICErel-III or TY) make up the Group I caspases, all of which prefer the tetrapeptide substrate sequence WEHD. Although Group I caspases are involved in inflammation through the maturation of pro-IL-1ß There is evidence suggesting that activation of Group I caspases induces apoptosis, although substrate specificity studies do not provide compelling evidence for a role of Group I caspases in apoptosis since hydrophobic amino acids in the P4 position (prefered by Group I) are not observed in proteins cleaved during apoptosis. Most research supports a role for Caspase-1 in inflammation but the roles of Caspase-4 and Caspase-5 have not been established.
Chemical Name Z-WEHD fluoromethylketone
Formula C₃₇H₄₂FN₇O₁₁
Solubility DMSO
Molecular Weight 877 Da
Comment

Dissolve Caspase-1,4,5 Inhibitor in high purity (99.9%) DMSO before use.

For use on intact cells:
1. Prepare desired concentrated stock solutions as follows:
1 mg Z-WEHD-FMK
in 5µl DMSO = 20 mM
in 114 µl DMSO = 10 mM
in 228 µl DMSO = 5 mM, etc.

2. Add 2µl of 10 mM stock solution to 1 ml culture medium containing cells such that the final concentration of DMSO is 0.2%. Levels of DMSO above this may cause some cellular toxicity, thus masking the effect of the Caspase-1,4,5 protease inhibitor. Adding 2 µl of a 10 mM stock solution to 1 ml of culture medium gives a final final Z-WEHD-FMK concentration of 20 µM. Typical final concentrations of inhibitor are 5-20 µM.

For extended use in vivo or in vitro:
For experiments extending 12 to 48 hours, fresh inhibitor may have to be added (injected) due to inactivation of the inhibitor by endogenous cysteine proteases.
IMPORTANT NOTE for in vitro use: Our peptide inhibitors are synthesized as methyl esters to enhance cell permeability. In intact cells, the methyl groups are removed by endogenous enzymes. For in vitro experiments with purified enzymes, however, the methyl groups must first be removed by treating the inhibitor with esterase.
Restrictions For Research Use only
Format Solid
Storage RT