Home Proteases Cysteine Protease inhibitor - COVID-19 inhibitor Aloxistatin (E64d) For research use only.

Aloxistatin (E64d)

Synonyms: E-64d

Aloxistatin (E64d) is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry, and aloxistatin treatment reduced cellular entry of SARS-CoV-2 pseudovirions by 92.3%.

Aloxistatin (E64d) Chemical Structure

Aloxistatin (E64d) Chemical Structure

CAS: 88321-09-9

Selleck's Aloxistatin (E64d) has been cited by 35 publications

Purity & Quality Control

Batch: Purity: 99.83%
99.83

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U937 cells Function assay Blockade of cathepsin G processing in human U937 cells by densitometry, IC50=1.1 μM 17535802
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Biological Activity

Description Aloxistatin (E64d) is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry, and aloxistatin treatment reduced cellular entry of SARS-CoV-2 pseudovirions by 92.3%.
Targets
Cysteine protease [1]
In vitro
In vitro

Aloxistatin can enter the intact platelet and inhibit proteolysis by inhibiting calpain. [2]

Aloxistatin blunts Parathyroid hormone (PTH)-induced cell proliferation and inhibits differentiation osteoblasts in vitro. [3]
Cell Research Cell lines NCM460 cells
Concentrations 1 μM
Incubation Time 24 h
Method

Cells were treated with indicated concentration of the drug for 24 hour.
Experimental Result Images Methods Biomarkers Images PMID
Western blot LAMP-1 / Rab5 / pro-Ctsl / Ctsl / Ctsb / pro-Ctsd 25744631
Immunofluorescence LAMP-1 25744631
In Vivo
In vivo

Aloxistatin (100 mg/kg, p.o.) strongly inhibits the cathepsin B&L activities in the skeletal muscle, heart and liver of hamsters. [1]

In spinal cord injury (SCI) rats, Aloxistatin provides neuroprotection in SCI lesion and penumbra. [4]

Aloxistatin reduces brain amyloid-β and improves memory deficits in Alzheimer's disease animal models by inhibiting cathepsin B activity. [5]
Animal Research Animal Models Hamsters
Dosages ~100 mg/kg
Administration p.o.

Chemical lnformation & Solubility

Molecular Weight 342.43 Formula

C17H30N2O5
CAS No. 88321-09-9 SDF Download Aloxistatin (E64d) SDF
Smiles CCOC(=O)C1C(O1)C(=O)NC(CC(C)C)C(=O)NCCC(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 68 mg/mL ( (198.58 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 68 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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