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| | CHYMOSTATIN Basic information |
| Product Name: | CHYMOSTATIN | | Synonyms: | (S)-1-CARBOXY-2-PHENYLETHYL]-CARBAMOYL-ALPHA-[2-AMIDOHEXAHYDRO-4(S)-PYRIMIDYL]-(S)-GLYCYL-[A = LEU; B = VAL; OR C = ILE]-PHENYLALANINAL;(S)-1-CARBOXY-2-PHENYLETHYL)-CARBAMOYL-ALPHA-[2-IMINOHEXAHYDRO-4(S)-PYRIMIDYL]-(S)-GLYCYL-X-PHENYLALANINAL;[(S)-1-CARBOXY-2-PHENYLETHYL]-CARBAMOYL-ALPHA-[2-IMINOHEXAHYDRO-4(S)-PYRIMIDYL]-(S)-GLY-X-PHE-AL;N-[-N-ALPHA-CARBONYL-CPD-X-PHE-AL]-PHE;CHYMOSTATIN;AIDS-028443;ChyMostatin research grade;N-(Nα-Carbonyl-Cpd-X-Phe-al)-Phe (Cpd = capreomycidine) (capreomycidine = [S,S]-α-(2-Iminohexahydro-4-pyrimidyl)glycine) | | CAS: | 9076-44-2 | | MF: | C92H121N21O18 | | MW: | 1809.08 | | EINECS: | 618-642-0 | | Product Categories: | peptides | | Mol File: | 9076-44-2.mol |  |
| | CHYMOSTATIN Chemical Properties |
| Melting point | 205 °C | | storage temp. | -20°C | | solubility | DMSO: 10 mM Stock solutions stable for months at −20 °C. | | form | White to slightly yellow solid or powder | | color | White or off-white | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| | CHYMOSTATIN Usage And Synthesis |
| Description | Chymostatin is a bioactive peptide of microbial origin that acts as a protease inhibitor with selectivity for chymotryptase-like serine proteases. It potently inhibits chymotrypsin and chymase (Ki = 9.36 and 13.1 nM, respectively) while less effectively blocking the activity of cathepsins, papain, and leukocyte elastase. It is without effect on trypsin, thrombin, plasmin, pepsin, and kallikrein. | | Uses | 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. | | Uses | Chymostatin is a specific inhibitor of α-, β-, γ-, and δ-chymotrypsin. | | General Description | Chymostatin is a mixture of three components, A, B, and C. The component A being N-[((S)-1-carboxy-2-phenylethyl)-carbamoyl]-α-[2-iminohexahydro-4(S)-pyrimidyl]-L-glycyl-L-leucyl-phenylalaninal. The other two components B and C differ in that the L-leucyl residue is substituted by L-valine and L-isoleucine, respectively. | | Biochem/physiol Actions | 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. | | in vitro | chymostatin was found to be a potent inhibitor of human leucocyte chymotrypsin-like protease. its affinity to the leucocyte protease was found to be much higher than its affinity to bovine pancreatic alpha-chymotrypsin. chymsotatin also showed a weak inhibitory effect on the activity of human leucocyte elastase. in addition, the preincubation of chymostatin with 35so2-4-labeled cartilage before the addition of the human chymotrypsin-like protease to the tissue could also inhibit 35so2-4 release [1]. | | in vivo | the effect of chymostatin on c57bl/6j-dy dystrophic mice was studied. the locomotor activity of normal mice markedly increased, attaining a plateau at 8 weeks of age. serum levels of creatine phosphokinase were much higher in dystrophic mice when compared with normal mice, and dystrophic mice also showed a reduced muscle protein content. when 3-week-old dystrophic mice received chymostatin at 1 mg/kg, the decrease in locomotor activity could be retarded, serum enzyme levels significantly decreased, and muscle protein content also obviously increased. in addition, the survival time of chymostatin-treated dystrophic mice was prolonged [2]. | | References | 1) Umezawa?et al.?(1970),?Chymostatin, a new chymotrypsin inhibitor produced by actinomycetes; J. Antibiot. (Tokyo)?23?425
2) Johnson?et al.?(1998),?Inactivation of chymotrypsin and human skin chymase: kinetics of time-dependent inhibition in the presence of substrate; Biochim. Biophys. Acta?953?269
3) Stein and Strimpler (1987),?Slow-binding of chymotrypsin and cathepsin G by the peptide aldehyde chymostatin; Biochemistry?26?2611
4) Roszkowska-Chojecka?et al.?(2015),?Effects of chymostatin, a chymase inhibitor, on blood pressure, plasma and tissue angiotensin II, renal haemodynamics and renal excretion in two models of hypertension in the rat; Exp. Physiol.?100?1093 |
| | CHYMOSTATIN Preparation Products And Raw materials |
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