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Merck

E8640

Sigma-Aldrich

E-64d

powder, ≥98% (TLC)

Sinónimos:

(2S,3S)-trans-Epoxysuccinyl-L-leucylamido-3-methylbutane ethyl ester, EST

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About This Item

Fórmula empírica (notación de Hill):
C17H30N2O5
Número de CAS:
Peso molecular:
342.43
MDL number:
UNSPSC Code:
12352202
PubChem Substance ID:
NACRES:
NA.77

product name

E-64d, protease inhibitor

biological source

synthetic (organic)

Quality Level

assay

≥98% (TLC)

form

powder

solubility

methanol: water (1:1): 5 mg/mL, clear, colorless

storage temp.

−20°C

SMILES string

CCOC(=O)[C@H]1O[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)NCCC(C)C

InChI

1S/C17H30N2O5/c1-6-23-17(22)14-13(24-14)16(21)19-12(9-11(4)5)15(20)18-8-7-10(2)3/h10-14H,6-9H2,1-5H3,(H,18,20)(H,19,21)/t12-,13-,14-/m0/s1

InChI key

SRVFFFJZQVENJC-IHRRRGAJSA-N

Gene Information

human ... CAPN1(823)

Application

E-64d has been used as a lysosomal inhibitor in human acute promyelocytic leukemia NB4 cells and Huh-7 cells. It has also been used as a protease inhibitor in free calcium physiological tyrode solution for perfusion into the isolated heart samples.

Biochem/physiol Actions

E-64d is an epoxysuccinyl peptide and an inhibitor of cysteine protease cathepsin B, calpains 1 and 2. E-64d by its cathepsin B protease inhibition functionality, may serve as a potential drug for treating traumatic brain injury (TBI) and Alzheimer′s disease (AD). It inhibits gametocyte surface antigen resulting in a decreased oocyst production in Plasmodium falciparum.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves


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The cysteine protease inhibitor, E64d, reduces brain amyloid-beta and improves memory deficits in Alzheimer's disease animal models by inhibiting cathepsin B, but not BACE1, beta-secretase activity
Hook G, et al.
Journal of Alzheimer'S Disease, 26(2), 387-408 (2011)
Inhibition of Plasmodium falciparum oocyst production by membrane-permeant cysteine protease inhibitor E64d
Eksi S, et al.
Antimicrobial Agents and Chemotherapy, 51(3), 1064-1070 (2007)
Mebrahtom Gebrelibanos Hiben et al.
Journal of ethnopharmacology, 241, 111978-111978 (2019-06-01)
Maerua subcordata (Gilg) DeWolf is a medicinal and wild food plant growing mainly in east Africa. Especially its root tuber is widely used in traditional medicine to treat several infectious and chronic diseases but also in some toxicity implications like
Cathepsin B is a new drug target for traumatic brain injury therapeutics: evidence for E64d as a promising lead drug candidate
Hook G, et al.
Frontiers in Neurology, 6(9), 178-178 (2015)
John P Lloyd et al.
Scientific reports, 9(1), 12122-12122 (2019-08-23)
Extensive transcriptional activity occurring in intergenic regions of genomes has raised the question whether intergenic transcription represents the activity of novel genes or noisy expression. To address this, we evaluated cross-species and post-duplication sequence and expression conservation of intergenic transcribed

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