Home Proteases Cysteine Protease inhibitor - Apoptosis related activator - Parasite inhibitor - Cathepsin B inhibitor E-64 For research use only.

E-64

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.

E-64 Chemical Structure

E-64 Chemical Structure

CAS No. 66701-25-5

Purity & Quality Control

E-64 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human red blood cells assessed as inhibition of ring-stage parasite growth after 48 hrs by flow cytometry, IC50=1.94μM 21295887
human red blood cells Antiplasmodial assay 48 hrs Antiplasmodial activity against ring stage Plasmodium falciparum W2 infected in human red blood cells after 48 hrs by flow cytometry, IC50=1.94μM 22071522
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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
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
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]
Animal Research Animal Models M5076 tumor bearing mice
Dosages --
Administration i.v.

Chemical Information & Solubility

Molecular Weight 357.41 Formula

C15H27N5O5
CAS No. 66701-25-5 SDF Download E-64 SDF
Smiles CC(C)CC(C(=O)NCCCCN=C(N)N)NC(=O)C1C(O1)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 71 mg/mL ( (198.65 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 9 mg/mL

Ethanol : 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. )

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.

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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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