E 64d

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Description: Cathepsin inhibitor; interferes with autolysosomal digestion
Chemical Name: (2S,3S)-3-[[[(1S)-3-Methyl-1-[[(3-methylbutyl)amino]carbonyl]butyl]amino]carbonyl]-2-oxiranecarboxylic acid ethyl ester
Purity: ≥98% (HPLC)
Citations (6)

Biological Activity for E 64d

E 64d is an inhibitor of cathepsins B and L; also thought to inhibit calpain. Inhibits lysosomal proteases and interferes with autolysosomal digestion when used in combination with pepstatin A (Cat. No. 1190). Lysosome and cell permeable. Also inhibits entry of SARS-Cov-2 (COVID-19) into Caco-2 and Vero cells in combination with Camostat mesylate (Cat.No. 3193) in vitro.

Technical Data for E 64d

M. Wt 342.43
Formula C17H30N2O5
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 88321-09-9
PubChem ID 65663
Smiles O=[C@@](N[C@H]([C@](NCCC(C)C)=O)CC(C)C)[C@H]1O[C@@H]1C(OCC)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for E 64d

Solvent Max Conc. mg/mL Max Conc. mM
ethanol 6.85 20

Preparing Stock Solutions for E 64d

The following data is based on the product molecular weight 342.43. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 14.6 mL 73.01 mL 146.02 mL
1 mM 2.92 mL 14.6 mL 29.2 mL
2 mM 1.46 mL 7.3 mL 14.6 mL
10 mM 0.29 mL 1.46 mL 2.92 mL

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Product Datasheets for E 64d

Certificate of Analysis / Product Datasheet
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References for E 64d

References are publications that support the biological activity of the product.

Kim et al (2008) Autophagy upregulation by inhibitors of caspase-3 and mTOR enhances radiotherapy in a mouse model of lung cancer. Autophagy 4 659 PMID: 18424912

Sato et al (2007) Autophagy is activated in colorectal cancer cells and contributes to the tolerance to nutrient deprivation. Cancer Res. 67 9677 PMID: 17942897

Tanada et al (2005) Lysosomal turnover, but not a cellular level, of endogenous LC3 is a marker for autophagy. Autophagy 1 84 PMID: 16874052

Wilcox and Mason (1992) Inhibition of cysteine proteinases in lysosomes and whole cells. Biochem.J. 285 495 PMID: 1637341

Hoffmann et al (2020) SARS-CoV-2 cell entry depends on ACE2 and TMPRSS2 and is blocked by a clinically-proven protease inhibitor. Cell 181 271 PMID: 32142651

If you know of a relevant reference for E 64d, please let us know.

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Keywords: E 64d, E 64d supplier, lysosomal, proteases, inhibitors, inhibits, cathepsins, autophagy, autolysosomal, digestion, E64d, COVID-19, SARS-Cov-2, Autophagy, Calcium-Sensitive, Proteases, Cathepsin, Coronavirus, 4545, Tocris Bioscience

6 Citations for E 64d

Citations are publications that use Tocris products. Selected citations for E 64d include:

Bo et al (2022) SARS-CoV-2 spike N-terminal domain modulates TMPRSS2-dependent viral entry and fusogenicity. Cell Rep 40 111220 PMID: 35963244

Arlene H et al (2022) PD-L1 promotes myofibroblastic activation of hepatic stellate cells by distinct mechanisms selective for TGF-β receptor I versus II. Cell Rep 38 110349 PMID: 35139382

Da-Yuan et al (2023) Cell culture systems for isolation of SARS-CoV-2 clinical isolates and generation of recombinant virus. iScience 26 106634 PMID: 37095858

Zhang et al (2017) TRPC5-induced autophagy promotes drug resistance in breast carcinoma via CaMKKβ/AMPKα/mTOR pathway. Sci Rep 7 3158 PMID: 28600513

Do you know of a great paper that uses E 64d from Tocris? Please let us know.

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