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Description: Calpain and cathepsin L inhibitor
Chemical Name: N-Benzyloxycarbonyl-L-leucylnorleucinal
Citations (10)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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:

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

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

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

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