Calpain Inhibitor

Nom chimique: (2S,3S)-trans-Epoxysuccinyl-L-leucylamido-3-methylbutane // Synonymes: E-64c, (2S,3S)-3-((S)-1-(isopentylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)oxirane-2-carboxylic acid

  • n° Art.:HAA3340
  • n° CAS:76684-89-4
  • Formule:C15H26N2O5
  • Storage temperature:-20°C
  • Masse moléculaire:314,38 g/mol

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description

Also known as E-64c, this potent inhibitor of calpain is a membrane-impermeable analog of E-64. It shows a higher inhibitory activity against cathepsins B and L compared to E-64 (LS-3890).

references

Structural basis of inhibition of cysteine proteases by E-64 and its derivatives; K. Matsumoto, K. Mizoue, K. Kitamura, W. C. Tse, C. P. Huber and T. Ishida; Biopolymers 1999; 51: 99-107. doi:10.1002/(SICI)1097-0282(1999)51:1<99::AID-BIP11>3.0.CO;2-R

Refined x-ray structure of papain.E-64-c complex at 2.1-A resolution; D. Yamamoto, K. Matsumoto, H. Ohishi, T. Ishida, M. Inoue, K. Kitamura and H. Mizuno; J Biol Chem 1991; 266: 14771-7.

Mode of binding of E-64-c, a potent thiol protease inhibitor, to papain as determined by X-ray crystal analysis of the complex; K. Matsumoto, D. Yamamoto, H. Ohishi, K. Tomoo, T. Ishida, M. Inoue, T. Sadatome, K. Kitamura and H. Mizuno; FEBS Letters 1989; 245: 177-180. doi:10.1016/0014-5793(89)80216-9


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