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E-64

Catalog No. T6037 CAS 66701-25-5

Synonyms: Proteinase inhibitor E 64, E 64, E64

E-64 (Proteinase inhibitor E 64) is an irreversible and specific cysteine protease inhibitor. The IC50 of E-64 for papain is 9 nM.

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E-64, CAS 66701-25-5

Pack Size	Availability	Price/USD
2 mg	In stock	$ 31.00
5 mg	In stock	$ 46.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 143.00
50 mg	In stock	$ 237.00
100 mg	In stock	$ 353.00
500 mg	In stock	$ 832.00
1 mL * 10 mM (in DMSO)	In stock	$ 47.00

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Purity: 99.95%

Purity: 99.66%

Purity: 99.65%

Purity: 99.47%

Purity: 99.29%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	E-64 (Proteinase inhibitor E 64) is an irreversible and specific cysteine protease inhibitor. The IC50 of E-64 for papain is 9 nM.
Targets&IC50	Cysteine protease: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]
Kinase Assay	The Cathepsin Β activity is determined using Z-Arg-Arg-4mβNA as substrate with slight modifications. The crude extract is pre-incubated at 37°C for 5 min in 50 mM sodium acetate buffer, pH 5.0 containing 1 mM EDTA and 5 mM DTT. The substrate (final concentration, 100 μM) is added to make the final assay volume of 1 mL. The reaction mixture is incubated at 37°C for 30 min. The reaction is terminated by adding equal volume of stopping reagent containing Fast Garnet GBC salt (1 mg/mL), 10 mM pHMB and 50 mM EDTA, pH 6.0. The extraction of product, β-napthylamine (β-NA), is carried out with n-butanol. After complete layer separation, the absorbance is measured in n-butanol layer and activity is calculated using molar extinction coefficient of β-napthylamine solution as 31.5 M/cm per sec at 520 nm. One unit of enzyme activity is defined as the amount of enzyme liberating 1 μmol of βNA per minute at 37°C. The half maximal inhibitory concentration (IC50) is calculated by plotting the graph between the different concentration of E-64 and the % inhibition in cathepsin B activity. Here, IC50 indicates the concentration of the E-64 required to inhibit the parasitic cathepsin B activity by half[2].

Synonyms	Proteinase inhibitor E 64, E 64, E64
Molecular Weight	357.41
Formula	C15H27N5O5
CAS No.	66701-25-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 9 mg/mL (25.2 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 66 mg/mL (184.7 mM)

References and Literature

1. Matsumoto K, et al. Biopolymers. 1999, 51(1), 99-107. 2. Barrett AJ, et al. Biochem J. 1982, 201(1), 189-198. 3. Kobayashi H, et al. Cancer Res. 1992, 52(13), 3610-3614. 4. Hussein EM, et al. J Egypt Soc Parasitol. 2009, 39(1), 111-119. 5. Min SH, et al. J Reprod Dev. 2014, 60(1), 21-27. 6. Blass G, et al. Chronic cathepsin inhibition by E-64 in Dahl salt-sensitive rats. Physiol Rep. 2016 Sep;4(17). pii: e12950. 7. Zhang B, Chen Z. Screening of cathepsin B inhibitors in traditional Chinese medicine by capillary electrophoresis with immobilized enzyme microreactor[J]. Journal of Pharmaceutical and Biomedical Analysis. 2019: 112811. 8. Jiang T Y, Pan Y F, Wan Z H, et al. PTEN status determines chemosensitivity to proteasome inhibition in cholangiocarcinoma[J]. Science Translational Medicine. 2020, 12(562).

Citations

1. Guan X N, Zhang T, Yang T, et al. Covalent Sortase A Inhibitor ML346 Prevents Staphylococcus aureus Infection of Galleria mellonella. RSC Medicinal Chemistry. 2022 2. Jiang T Y, Pan Y F, Wan Z H, et al. PTEN status determines chemosensitivity to proteasome inhibition in cholangiocarcinoma. Science Translational Medicine. 2020, 12(562). 3. Zhang B, Chen Z. Screening of cathepsin B inhibitors in traditional Chinese medicine by capillary electrophoresis with immobilized enzyme microreactor. Journal of Pharmaceutical and Biomedical Analysis. 2019: 112811

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Preclinical Compound Library Anti-Bacterial Compound Library Apoptosis Compound Library Anti-COVID-19 Compound Library Anti-Cancer Compound Library Protease Inhibitor Library

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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.

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Keywords

E-64 66701-25-5 Autophagy Microbiology/Virology Proteases/Proteasome Cysteine Protease Antibacterial Proteinase inhibitor E 64 Cathepsin E 64 Inhibitor Proteinase inhibitor E-64 inhibit Proteinase inhibitor E64 E64 Bacterial inhibitor

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