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Submit ReviewCA 074
Description: Selective cathepsin B inhibitor
Chemical Name: N-[[(2S,3S)-3-[(Propylamino)carbonyl]-2-oxiranyl]carbonyl]-L-isoleucyl-L-proline
Purity: ≥98% (HPLC)
Biological Activity
Inhibitor of cathepsin B (Ki = 2-5 nM). Displays selectivity over cathepsins H and L (Ki = 40-200 μM). Shown to reduce bone metastasis in a 4T1.2 breast cancer model.
Technical Data
| M. Wt | 383.44 |
| Formula | C18H29N3O6 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 134448-10-5 |
| PubChem ID | 9821383 |
| InChI Key | ZEZGJKSEBRELAS-PEDHHIEDSA-N |
| Smiles | O=[C@](NCCC)[C@H]1O[C@@H]1[C@@](N[C@@H]([C@@H](C)CC)[C@](N2[C@H](C(O)=O)CCC2)=O)=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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.67 | 20 | |
| ethanol | 7.67 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 383.44. 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 | 13.04 mL | 65.2 mL | 130.4 mL |
| 1 mM | 2.61 mL | 13.04 mL | 26.08 mL |
| 2 mM | 1.3 mL | 6.52 mL | 13.04 mL |
| 10 mM | 0.26 mL | 1.3 mL | 2.61 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Gillet et al (2009) Voltage-gated sodium channel activity promotes cysteine cathepsin-dependent invasiveness and colony growth of human cancer cells. J.Biol.Chem. 284 8680 PMID: 19176528
Towatari et al (1991) Novel epoxysuccinyl peptides. A selective inhibitor of cathepsin B, in vivo. FEBS Lett. 280 311 PMID: 2013329
Withana et al (2012) Cathepsin B inhibition limits bone metastasis in breast cancer. Cancer Res. 72 1199 PMID: 22266111
If you know of a relevant reference for CA 074, please let us know.
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Keywords: CA 074, CA 074 supplier, CA074, cathepsin, B, selective, inhibitors, inhibits, cysteine, proteases, Cathepsin, Calcium-Sensitive, Proteases, 4863, Tocris Bioscience
1 Citation for CA 074
Citations are publications that use Tocris products. Selected citations for CA 074 include:
Li et al (2018) C. elegans-based screen identifies lysosome-damaging alkaloids that induce STAT3-dependent lysosomal cell death. Protein Cell 9 1013 PMID: 29611115
Do you know of a great paper that uses CA 074 from Tocris? Please let us know.
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