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Aloxistatin (E-64d) Cysteine Protease inhibitor

Name: Aloxistatin (E-64d)
Brand: Selleck Chemicals
SKU: S7393
Rating: 5 (47 reviews)

Cat.No.S7393

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%.

Chemical Structure

Molecular Weight: 342.43

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Quality Control

Batch: Purity: 99.83%

99.83

Related Targets	HDAC Caspase Proteasome Secretase MMP HCV Protease DPP Tyrosinase HIV Protease Serine Protease
Other Cysteine Protease Inhibitors	N-Ethylmaleimide (NEM) MG132 SSS Calpeptin Odanacatib E-64 MG-101 (ALLN) Z-FA-FMK Cathepsin Inhibitor 1 PD 151746 Loxistatin Acid (E-64C)

Cell Culture, Treatment & Working Concentration

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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	342.43	Formula	C₁₇H₃₀N₂O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	88321-09-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	E-64d			Smiles	CCOC(=O)C1C(O1)C(=O)NC(CC(C)C)C(=O)NCCC(C)C

Solubility

In vitro
Batch:

DMSO : 68 mg/mL (198.58 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 68 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Cysteine protease
In vitro	Aloxistatin (E64d) can enter the intact platelet and inhibit proteolysis by inhibiting calpain. It blunts Parathyroid hormone (PTH)-induced cell proliferation and inhibits differentiation osteoblasts in vitro.
In vivo	Aloxistatin (E64d) (100 mg/kg, p.o.) strongly inhibits the cathepsin B&L activities in the skeletal muscle, heart and liver of hamsters. In spinal cord injury (SCI) rats, it provides neuroprotection in SCI lesion and penumbra. This compound reduces brain amyloid-β and improves memory deficits in Alzheimer's disease animal models by inhibiting cathepsin B activity.
References	[1] https://pubmed.ncbi.nlm.nih.gov/3023601/ [2] https://pubmed.ncbi.nlm.nih.gov/2537073/ [3] https://pubmed.ncbi.nlm.nih.gov/9284902/ [4] https://pubmed.ncbi.nlm.nih.gov/11462799/ [5] https://pubmed.ncbi.nlm.nih.gov/21613740/ [6] https://pubmed.ncbi.nlm.nih.gov/35974017/

Applications

Methods	Biomarkers	Images	PMID
Western blot	LAMP-1 / Rab5 / pro-Ctsl / Ctsl / Ctsb / pro-Ctsd		25744631
Immunofluorescence	LAMP-1		25744631

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Handling Instructions

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