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Description: Calpain and cathepsin L inhibitor
Chemical Name: N-Benzyloxycarbonyl-L-leucylnorleucinal
Biological Activity for Calpeptin
Calpeptin is a potent, cell-permeable inhibitor of the Ca2+-dependent protease, calpain. Prevents collagen- and thrombin-induced platelet aggregation, probably by blocking calpain induced phospholipase C and thromboxane synthase activation. Potent cathepsin L inhibitor. Recently shown to preferentially inhibit a subset of protein-tyrosine phosphatases. Also inhibits SARS-CoV-2 Mpro in vitro (IC50 = 10.7 μM) and inhibits viral replication.
Technical Data for Calpeptin
| M. Wt | 362.47 |
| Formula | C20H30N2O4 |
| Storage | Desiccate at +4°C |
| CAS Number | 117591-20-5 |
| PubChem ID | 73364 |
| InChI Key | PGGUOGKHUUUWAF-ROUUACIJSA-N |
| Smiles | O=C(OCC1=CC=CC=C1)N[C@H](C(N[C@H](C([H])=O)CCCC)=O)CC(C)C |
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 Calpeptin
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 100 |
Preparing Stock Solutions for Calpeptin
The following data is based on the product molecular weight 362.47. 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 |
|---|---|---|---|
| 1 mM | 2.76 mL | 13.79 mL | 27.59 mL |
| 5 mM | 0.55 mL | 2.76 mL | 5.52 mL |
| 10 mM | 0.28 mL | 1.38 mL | 2.76 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
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Product Datasheets for Calpeptin
References for Calpeptin
References are publications that support the biological activity of the product.
Mehdi (1991) Cell-penetrating inhibitors of calpain. TiBS 16 150 PMID: 1877091
Sasaki et al (1990) Inhibitory effect of di-and tripeptidyl aldehydes on calpains and cathepsins. J.Enzyme Inhib. 3 195 PMID: 2079636
Schoenwaelder and Burridge (1999) Evidence for a calpeptin-sensitive protein-tyrosine phosphatase upstream of the small GTPase Rho. J.Biol.Chem. 274 14359 PMID: 10318859
Tsujinaka et al (1988) Synthesis of a new cell penetrating calpain inhibitor (calpeptin). Biochem.Biophys.Res.Commun. 153 1201 PMID: 2839170
Ma et al (2020) Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main protease. Cell Res. 30 678 PMID: 32541865
If you know of a relevant reference for Calpeptin, please let us know.
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Keywords: Calpeptin, Calpeptin supplier, Calpain, cathepsin, L, inhibitors, inhibits, Proteinases, Proteases, Ca2+Sensitive, Protease, modulators, Calcium-Sensitive, Ca2+, Signaling, Signalling, Calpains, Cathepsin, 3C, and, 3CL, 0448, Tocris Bioscience
10 Citations for Calpeptin
Citations are publications that use Tocris products. Selected citations for Calpeptin include:
Zakharova et al (2015) Platelet surface-associated activation and secretion-mediated inhibition of coagulation factor XII. PLoS One 10 e0116665 PMID: 25688860
Amadoro et al (2006) NMDA receptor mediates tau-induced neurotoxicity by calpain and ERK/MAPK activation. Proc Natl Acad Sci U S A 103 2892 PMID: 16477009
Zhou and Cai (2019) Calpeptin Reduces Neurobehavioral Deficits and Neuronal Apoptosis Following Subarachnoid Hemorrhage in Rats. J Stroke Cerebrovasc Dis 28 125 PMID: 30337208
Leytin et al (2009) Mitochondrial control of platelet apoptosis: effect of cyclosporin A, an inhibitor of the mitochondrial permeability transition pore. Lab Invest 89 374 PMID: 19238135
Machado et al (2015) Involvement of calpains in adult neurogenesis: implications for stroke. J Biol Chem 9 22 PMID: 25698931
Wang et al (2015) MFN2 couples glutamate excitotoxicity and mitochondrial dysfunction in motor neurons. J Pharmacol Exp Ther 290 168 PMID: 25416777
Santos et al (2012) Distinct regulatory functions of calpain 1 and 2 during neural stem cell self-renewal and differentiation. PLoS One 7 e33468 PMID: 22432027
Redpath et al (2014) Calpain cleavage within dysferlin exon 40a releases a synaptotagmin-like module for membrane repair. Mol Biol Cell 25 3037 PMID: 25143396
Rivera-Pagán et al (2015) Up-regulation of TREK-2 potassium channels in cultured astrocytes requires de novo protein synthesis: relevance to localization of TREK-2 channels in astrocytes after transient cerebral ischemia. PLoS One 10 e0125195 PMID: 25886567
Chen et al (2013) Nerve injury increases GluA2-lacking AMPA receptor prevalence in spinal cords: functional significance and signaling mechanisms. Pflugers Arch 347 765 PMID: 24030012
Do you know of a great paper that uses Calpeptin from Tocris? Please let us know.
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