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Submit ReviewE 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.
M. Wt | 342.43 |
Formula | C17H30N2O5 |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 88321-09-9 |
PubChem ID | 65663 |
InChI Key | SRVFFFJZQVENJC-IHRRRGAJSA-N |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
ethanol | 6.85 | 20 |
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.
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 |
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.
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
Citations are publications that use Tocris products. Selected citations for E 64d include:
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
Guerroue et al (2017) Autophagosomal Content Profiling Reveals an LC3C-Dependent Piecemeal Mitophagy Pathway. Mol Cell 68 786 PMID: 29149599
Yingqiong et al (2021) A simple protocol to produce mature human-induced pluripotent stem cell-derived cardiomyocytes. STAR Protoc 2 100912 PMID: 34755117
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
Do you know of a great paper that uses E 64d from Tocris? Please let us know.
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