Ligand E-64d

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Basic Ligand Information

Molecular Structure
Picture of E-64d (click for magnification)
Molecular Formula
BRENDA Name
InChIKey
C17H30N2O5
E-64d
SRVFFFJZQVENJC-IHRRRGAJSA-N
Synonyms:
(2S,3S)-trans-epoxysuccinyl-L-leucylamido-3-methylbutane ethyl ester, E-64-d, E64d, ethyl (2S,3S)-3-(((1S)-3-methyl-1-[(3-methylbutyl)carbamoyl]butyl)carbamoyl)oxirane-2-carboxylate, ethyl(2S,3S)-3-(S)-3-methyl-1-(3-methylbutylcarbamoyl)butylcarbamoyl oxirane-2-carboxylate, L-trans-epoxysuccinyl-(ethoxy)-Leu-3-methylbutylamide ethyl ester

Roles as Enzyme Ligand

Inhibitor in Enzyme-catalyzed Reactions (25 results)

EC NUMBER
COMMENTARY
LITERATURE
ENZYME 3D STRUCTURE
i.e. E64d, inhibits cell growth and is cytopathic/lethal for E64-sensitive and E64-resistant amoebae
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the caspase-1 activation is inhibited by E-64d, marked inhibition at 0.05 mM
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0.01 mM, 50% inhibition
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membrane-permeable do the irreversible cysteine proteinase inhibitor E-64 blocks cleavage of p65 in vivo
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treatment of London APP transgenic mouse model of Alzheimer's disease that expresses human amyloid precursor protein containing the wild-type beta-secretase site results in substantial improvement in memory deficit assessed by the Morris water maze test. Improved memory function is accompanied by reduced amyloid plaque load, decreased amyloid beta40 and amyloid beta42, and reduced C-terminal beta-secretase fragment derived from amyloid precursor protein by beta-secretase. Inhibitor has no effects on any of these parameters in mice expressing the Swedish mutant beta-secretase site of amyloid precursor protein
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0.1 mM, 30% inhibition of hydrolysis of succinyl-Leu-leu-Val-Tyr-7-amido-4-methylcoumarin, no inhibition of hydrolysis of tert-butyloxycarbonyl-Phe-Ser-Arg-7-amido-4-methylcoumarin, benzyloxycarbonyl-Leu-Leu-Leu-7-amido-4-methylcoumarin, benzyloxycarbonyl-Leu-Leu-Glu-7-amido-4-methylcoumarin
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Enzyme Kinetic Parameters

References & Links

Links to other databases for E-64d

ChEBI
PubChem
ChEBI
PubChem