Synonym: N-(Nα-Carbonyl-Cpd-X-Phe-al)-Phe (Cpd = capreomycidine) (capreomycidine = [S,S]-α-(2-Iminohexahydro-4-pyrimidyl)glycine)
|Related Categories||A to C, Apoptosis Enzymes, Application Index, Bioactive Small Molecules, Biochemicals and Reagents,|
|solubility||DMSO: soluble10 mM (Stock solutions stable for months at −20 °C.)|
Chymostatin is a strong inhibitor of many proteases, including chymotrypsin, papain, chymotrypsin-like serine proteinases, chymases, and lysosomal cysteine proteinases such as cathepsins A,B,C, B, H, and L. It weakly inhibits human leucocyte elastase. It is effective at a final concentration of 100 to 200 μg/ml (10 to 100 μM). Chymostatin is often included in protease inhibitor cocktails used with plant extracts.
Inhibits the lysosomal proteinase cathepsin B, and the soluble Ca2+-activated proteinase.1 Many young plant tissues express a chomostatin-sensitive serine protease.2
A mixture of A (major), B and C components. A: X=Leu; B: X=Val; C: X=Ile
chymostatin A MW = 607.7
chymostatin B MW = 593.7
chymostatin C MW = 607.7
Solubility testing in glacial acetic acid at 10 mg/ml yields a clear solution, which is usually colorless, but can be yellow in appearance. It is reportedly also soluble in DMSO; only slightly soluble in water and short-chain alcohols; insoluble in ethyl acetate, butyl acetate, ether, hexane, and petroleum ether. Stock solutions (10 mM) can be prepared in DMSO and are stable for months at -20 °C. Stock solutions can also be made in 0.1 M HCl. Dilute solutions (10-100 μM) are only stable for several hours, due to oxidation of the terminal aldehyde.
Chymostatin has been used in a study that determined that molecular calculations are useful for evaluating the interactions between ligands, including inhibitors and homologous enzymes, in docking models. Chymostatin has also been used in a study to investigate the norovirus protease as an attractive target for antiviral drug development.
Certificate of Analysis
Certificate of Origin
Beynon, R.J. and Bond, J.S., ed. Proteolytic Enzymes: A Practical Approach New York, NY , (1989), 207,243
Levy, M.R. and Chou, S.C. Biochim. Biophys. Acta 334, 423, (1974)
Comparative analysis of binding energy of chymostatin with human cathepsin A and its homologous proteins by molecular orbital calculation Yoshida, T., et al. J. Chem. Inf. Model. 46, 2093-103, (2012)
Cordysobin, a novel alkaline serine protease with HIV-1 reverse transcriptase inhibitory activity from the medicinal mushroom Cordyceps sobolifera Wang, S., et al. J. Biosci. Bioeng. 113(1), 42-7, (2011)
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