| Identification | Back Directory | [Name]
CHYMOSTATIN | [CAS]
9076-44-2 | [Synonyms]
CHYMOSTATIN
AIDS-028443
CHYMOSTATIN USP/EP/BP
ChyMostatin research grade
ACRYLAMIDE PROTEOMICS GRADE
Chymostatin from Microbial Source
chymostatin, mixture of components A
N-[-N-ALPHA-CARBONYL-CPD-X-PHE-AL]-PHE
Chymostatin - CAS 9076-44-2 - Calbiochem
CHYMOSTATIN, MIXTURE OF COMPONENTS A, B AND C
N-[-Nα-carbonyl-[S,S]-α-(2-iminohexahydro-4-pyrimidyl)glycine-Val-Phe-al]-Phe
[(S)-1-CARBOXY-2-PHENYLETHYL]-CARBAMOYL-ALPHA-[2-IMINOHEXAHYDRO-4(S)-PYRIMIDYL]-(S)-GLY-X-PHE-AL
(S)-1-CARBOXY-2-PHENYLETHYL)-CARBAMOYL-ALPHA-[2-IMINOHEXAHYDRO-4(S)-PYRIMIDYL]-(S)-GLYCYL-X-PHENYLALANINAL
N-(Nα-Carbonyl-Cpd-X-Phe-al)-Phe (Cpd = capreomycidine) (capreomycidine = [S,S]-α-(2-Iminohexahydro-4-pyrimidyl)glycine)
n-(nα-carbonyl-cpd-x-phe-al)-phe (cpd = capreomycidine) (capreomycidine = [s,s]-α-(2-iminohexahydro-4-pyrimidyl)glycine)
(S)-1-CARBOXY-2-PHENYLETHYL]-CARBAMOYL-ALPHA-[2-AMIDOHEXAHYDRO-4(S)-PYRIMIDYL]-(S)-GLYCYL-[A = LEU; B = VAL; OR C = ILE]-PHENYLALANINAL
(2S)-2-[[(1S)-1-(2-Amino-3,4,5,6-tetrahydropyrimidin-4-yl)-2-[[(2S)-4-methyl-1-oxo-1-[[(2S)-1-oxo-3-phenylpropan-2-yl]amino]pentan-2-yl]amino]-2-oxoethyl]carbamoylamino]-3-phenylpropanoic acid | [EINECS(EC#)]
618-642-0 | [Molecular Formula]
C92H121N21O18 | [MDL Number]
MFCD00071059 | [MOL File]
9076-44-2.mol | [Molecular Weight]
1809.08 |
| Chemical Properties | Back Directory | [Melting point ]
276-278℃ | [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. |
| Hazard Information | Back Directory | [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]
Inhibitor of serine proteinases having a chymotrypsin-like specificity like α-, β-, δ- and γ-chymotrypsin, chymases, cathepsin G, and most cysteine proteinases including papain and cathepsin A, B, H, and L. Mixture of type A (R=L-Leu), type B (R=L-Val), type C (R=L-Ile). | [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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