Aloxistatin (E64d)

Catalog No.S7393 Batch:S739303

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Technical Data

Formula

C17H30N2O5

Molecular Weight 342.43 CAS No. 88321-09-9
Solubility (25°C)* In vitro DMSO 68 mg/mL (198.58 mM)
Ethanol 68 mg/mL (198.58 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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]

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 (from reference)

Cell Assay:

[6]

  • Cell lines

    NCM460 cells

  • Concentrations

    1 μM

  • Incubation Time

    24 h

  • Method

    Cells were treated with indicated concentration of the drug for 24 hour.

Animal Study:

[1]

  • Animal Models

    Hamsters

  • Dosages

    ~100 mg/kg

  • Administration

    p.o.

Selleck's Aloxistatin (E64d) has been cited by 39 publications

Truncating NFKB1 variants cause combined NLRP3 inflammasome activation and type I interferon signaling and predispose to necrotizing fasciitis [ Cell Rep Med, 2024, 5(4):101503] PubMed: 38593810
Retinoic acid alleviates rotavirus-induced intestinal damage by regulating redox homeostasis and autophagic flux in piglets [ Anim Nutr, 2024, 20:16:409-421.] PubMed: 38371474
A bat MERS-like coronavirus circulates in pangolins and utilizes human DPP4 and host proteases for cell entry [ Cell, 2023, 186(4):850-863.e16] PubMed: 36803605
Differences in syncytia formation by SARS-CoV-2 variants modify host chromatin accessibility and cellular senescence via TP53 [ Cell Rep, 2023, 42(12):113478] PubMed: 37991919
Cysteinyl leukotriene receptor 1 is a potent regulator of the endosomal-lysosomal system in the ARPE-19 retinal pigment epithelial cell line [ Traffic, 2023, 24(4):177-189] PubMed: 36704929
Canine distemper virus N protein induces autophagy to facilitate viral replication [ BMC Vet Res, 2023, 19(1):60] PubMed: 36922800
Canine distemper virus N protein induces autophagy to facilitate viral replication [ BMC Vet Res, 2023, 19(1):60] PubMed: 36922800
Babesia divergens egress from host cells is orchestrated by essential and druggable kinases and proteases [ Res Sq, 2023, rs.3.rs-2553721] PubMed: 36909484
Spike-mediated ACE2 down-regulation was involved in the pathogenesis of SARS-CoV-2 infection [ J Infect, 2022, S0163-4453(22)00404-2] PubMed: 35793758
RNF43G659fs is an oncogenic colorectal cancer mutation and sensitizes tumor cells to PI3K/mTOR inhibition [ Nature Communications, 2022, 3181-2022)] PubMed: None

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.