Aloxistatin(E64d)

For research use only.

Catalog No.S7393 Synonyms: E-64d

6 publications

Aloxistatin(E64d) Chemical Structure

Molecular Weight(MW): 342.43

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%.

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Choose Selective Cysteine Protease Inhibitors

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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U937 cells MljaSpVv[3Srb36gZZN{[Xl? NEfzXWhDdG:la3Hk[UBw\iClYYTo[ZB{cW5iRzDwdo9k\XO|aX7nJIlvKGi3bXHuJHU6OzdiY3XscJMh[nliZHXud4l1d22ndIL5MEBKSzVyPUGuNUDPxE1? Ml\mNVc2OzV6MEK=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
LAMP-1 / Rab5 / pro-Ctsl / Ctsl / Ctsb / pro-Ctsd ; 

PubMed: 25744631     


(B) Lamp-1, Rab5 Ctsl, Ctsb, and Ctsd protein levels were analyzed by Western blot with α-tubulin and actin as loading controls in whole cell lysates of untreated −/+E64d and four days TGFβ-1 −/+E64d treated iPL32 cells. Ctsl heavy (h) and light (l) chains indicate the fully processed mature protease.

25744631
Immunofluorescence
LAMP-1 ; 

PubMed: 25744631     


(A) Representative Lamp-1 immunofluorescence images of untreated −/+E64d and four days TGFβ-1 −/+E64d treated iPL32 cells are shown (Lamp-1: green, Hoechst nuclear stain: blue). 

25744631
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]

Protocol

Animal Research:

[1]

- Collapse
  • Animal Models: Hamsters
  • Dosages: ~100 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 68 mg/mL (198.58 mM)
Water Insoluble
Ethanol '''68 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+corn oil
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 342.43
Formula

C17H30N2O5

CAS No. 88321-09-9
Storage powder
in solvent
Synonyms E-64d
Smiles CCOC(=O)C1C(O1)C(=O)NC(CC(C)C)C(=O)NCCC(C)C

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID