E-64

Catalog No.S7379 Batch:S737910

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Technical Data

Formula

C15H27N5O5
Molecular Weight 357.41 CAS No. 66701-25-5
Solubility (25°C)* In vitro DMSO 71 mg/mL (198.65 mM)
Water 20 mg/mL (55.95 mM)
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.55mg/ml
* <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.)

Preparing Stock Solutions

Biological Activity

Description E-64 is an irreversible and selective cysteine protease inhibitor, and also inhibits papain, calpain, and cathepsins B and H, but not serine proteases or aspartic proteases. The IC50 for papain is 9 nM. E-64 induces oxidative stress and apoptosis in Filarial Parasite.
Targets
Cysteine protease [1]
(Cell-free assay)
9 nM
In vitro

E-64 rapidly inhibits the activities of the cysteine proteinases cathepsins B, H and L and papain, while has no effect on the serine proteinases or the metalloproteinases. [2]

E-64, as a specific inhibitor os cysteine proteases, effectively blocks in vitro ovarian cancer cell invasion. [3]

In addition, E-64 also shows antiparasitic activity against Giardia lamblia excystation in vitro. [4]

E-64 improves the preimplantation development of bovine somatic cell nuclear transfer embryos, which indicates another important implication of E-64. [5]
In vivo

E-64 induces a marked decrease in the number of spontaneous metastasis in M5076 tumor bearing mice, while has no effect on the formation of experimental metastasis. [6]

E-64 also shows antiparasitic activity against Giardia lamblia excystation in infected mice. [4]

Protocol (from reference)

Animal Study:

[5]
  • Animal Models

    M5076 tumor bearing mice

  • Dosages

    --

  • Administration

    i.v.

Selleck's E-64 has been cited by 17 publications

Acquired semi-squamatization during chemotherapy suggests differentiation as a therapeutic strategy for bladder cancer [ Cancer Cell, 2022, 40(9):1044-1059.e8] PubMed: 36099882
The Antagonizing Role of Heme in the Antimalarial Function of Artemisinin: Elevating Intracellular Free Heme Negatively Impacts Artemisinin Activity in Plasmodium falciparum [ Molecules, 2022, 27(6)1755] PubMed: 35335120
A lysosome-targeted DNA nanodevice selectively targets macrophages to attenuate tumours [ Nat Nanotechnol, 2021, 10.1038/s41565-021-00988-z] PubMed: 34764452
Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2 [ Cell Chem Biol, 2021, S2451-9456(21)00213-0] PubMed: 33979649
MMP-2 is a novel histone H3 N-terminal protease necessary for myogenic gene activation [ Epigenetics Chromatin, 2021, 14(1):23] PubMed: 34001241
Small molecule inhibitor E-64 exhibiting the activity against African swine fever virus pS273R [ Bioorg Med Chem, 2021, 35:116055] PubMed: 33607487
Evaluation of enzymatic proteoglycan loss and collagen degradation in human articular cartilage using ultrashort echo time-based biomarkers: A feasibility study [ NMR Biomed, 2021, e4664] PubMed: 34904305
The translocon-associated protein (TRAP) complex regulates quality control of N-linked glycosylation during ER stress [ Sci Adv, 2021, 7(3)eabc6364] PubMed: 33523898
FSGS-Causing INF2 Mutation Impairs Cleaved INF2 N-Fragment Functions in Podocytes. [ J Am Soc Nephrol, 2020, 31(2):374-391] PubMed: 31924668
Mechanism for enhanced transduction of hematopoietic cells by recombinant adeno-associated virus serotype 6 vectors [ FASEB J, 2020, 34(9):12379-12391] PubMed: 32960474

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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.

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