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E-64 Cysteine Protease inhibitor

Name: E-64
Brand: Selleck Chemicals
SKU: S7379
Availability: InStock
Rating: 5 (19 reviews)

Cat.No.S7379

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. This compound induces oxidative stress and apoptosis in Filarial Parasite.

Chemical Structure

Molecular Weight: 357.41

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	HDAC Caspase MMP HCV Protease DPP Tyrosinase HIV Protease Proteasome Serine Protease Secretase PCSK9 Glutaminase Acyltransferase Thrombin Cathepsin B MALT PAD PREP Neprilysin SGK Aminopeptidase 3C-Like Protease PGDS GOT
Related Products	Aloxistatin (E64d) Calpeptin Odanacatib MG-101 (ALLN) Z-FA-FMK N-Ethylmaleimide (NEM) Cathepsin Inhibitor 1 PD 151746 Loxistatin Acid (E-64C) Cruzain-IN-1 Z-FY-CHO Anti-CTSS / Cathepsin S (Fsn0503h) PD 150606 Cathepsin S Antibody [D17A22] LY3000328 MG132 SSS Calpain 1 Antibody [A6K6] Balicatib Calpain 2 Large Subunit (M-type) Antibody [K24F11] 2-cyano-Pyrimidine Cathepsin G Inhibitor I

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	357.41	Formula	C₁₅H₂₇N₅O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	66701-25-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C)CC(C(=O)NCCCCN=C(N)N)NC(=O)C1C(O1)C(=O)O

Solubility

In vitro
Batch:

DMSO : 71 mg/mL (198.65 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 9 mg/mL

Ethanol : 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.
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.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.550mg/ml (9.93mM)
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 ^[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] This compound, as a specific inhibitor os cysteine proteases, effectively blocks in vitro ovarian cancer cell invasion. ^[3] In addition, it also shows antiparasitic activity against Giardia lamblia excystation in vitro. ^[4] The chemical 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] This compound also shows antiparasitic activity against Giardia lamblia excystation in infected mice. ^[4]
References	[1] https://pubmed.ncbi.nlm.nih.gov/10380357/ [2] https://pubmed.ncbi.nlm.nih.gov/7044372/ [3] https://pubmed.ncbi.nlm.nih.gov/1617632/ [4] https://pubmed.ncbi.nlm.nih.gov/19530614/ [5] https://pubmed.ncbi.nlm.nih.gov/24240170/ [6] https://pubmed.ncbi.nlm.nih.gov/7919127/

Tech Support

Handling Instructions

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