CHYMOSTATIN
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.
Safety Information
- Hazard Codes
- Xi
- Risk Statements
- 36/37/38
- Safety Statements
- 22-24/25-36-26
- WGK Germany
- 3
- RTECS
- GC3047700
- F
- 10-21
MSDS
- Language:English Provider:SigmaAldrich
CHYMOSTATIN Usage And Synthesis
Description
Chymostatin is a bioactive peptide of microbial origin that acts as a protease inhibitor with selectivity for chymotryptase-
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
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