钙蛋白酶抑制剂VI是细胞可渗透的肽醛,其起可逆钙蛋白酶抑制剂的作用。研究表明,钙蛋白酶抑制剂VI强烈抑制组织蛋白酶B和组织蛋白酶L。此外,钙蛋白酶抑制剂VI降低了A23187诱导的核不透明性以及结晶蛋白和α-血影蛋白的蛋白水解作用。研究表明,在P1位置取代,特别是庞大的氨基酸残基醛,将增加钙蛋白酶抑制剂VI的效力。此外,钙蛋白酶抑制剂VI的S-构型在抑制组织蛋白酶L中很重要。 Calpain Inhibitor VI is a cell permeable peptide aldehyde which functions as a reversible calpain inhibitor. Studies indicate that Calpain Inhibitor VI strongly inhibits cathepsin B and cathepsin L. In addition, Calpain Inhibitor VI reduces nuclear opacity and proteolysis of crystallins and α-spectrin induced by A23187 . Studies suggest that substitution at the P1 position, specially a bulky amino acid residual aldehyde, will increase the potency of the Calpain Inhibitor VI. Furthermore, the S-configuration of Calpain Inhibitor VI is important in the inhibition of cathepsin L.
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Calpain Inhibitor VI
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| Chinese alias | 钙蛋白酶抑制剂 VI | ||
| English alias | N-(4-Fluorophenylsulfonyl)-L-Valyl-L-Leucinal | 2-[(4-fluorophenyl)sulfonylamino]-3-methyl-N-(4-methyl-1-oxopentan-2-yl)butanamide | DTXSID80622709 | N~2~-(4-Fluorobenzene-1-sulfonyl)-N-(4-methyl-1-oxopentan-2-yl)valinamide | ||
| CAS number | unknown | molecular formula | |
| molecular weight | - | Exact mass | ≥95% |
| PSA | - | logp | - |
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