Calpeptin (CAS 117591-20-5): R&D Systems
Catalog Number: 0448
Chemical Name: N-Benzyloxycarbonyl-L-leucylnorleucinal
Biological Activity
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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO
  • Storage:
    Desiccate at +4°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Evidence for a calpeptin-sensitive protein-tyrosine phosphatase upstream of the small GTPase Rho.
    Schoenwaelder and Burridge
    J.Biol.Chem., 1999;274:14359
  2. Synthesis of a new cell penetrating calpain inhibitor (calpeptin).
    Tsujinaka et al.
    Biochem.Biophys.Res.Commun., 1988;153:1201
  3. Cell-penetrating inhibitors of calpain.
    TiBS, 1991;16:150
  4. Inhibitory effect of di-and tripeptidyl aldehydes on calpains and cathepsins.
    Sasaki et al.
    J.Enzyme Inhib., 1990;3:195

The citations listed below are publications that use Tocris products. Selected citations for Calpeptin include:

6 Citations: Showing 1 - 6
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  1. Involvement of calpains in adult neurogenesis: implications for stroke.
    Authors: Machado Et al.
    J Biol Chem 2015;9:22
  2. MFN2 couples glutamate excitotoxicity and mitochondrial dysfunction in motor neurons.
    Authors: Wang Et al.
    J Pharmacol Exp Ther 2015;290:168
  3. 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.
    Authors: Rivera-Pagán Et al.
    PLoS One 2015;10:e0125195
  4. Calpain cleavage within dysferlin exon 40a releases a synaptotagmin-like module for membrane repair.
    Authors: Redpath Et al.
    Mol Biol Cell 2014;25:3037
  5. Nerve injury increases GluA2-lacking AMPA receptor prevalence in spinal cords: functional significance and signaling mechanisms.
    Authors: Chen Et al.
    Pflugers Arch 2013;347:765
  6. NMDA receptor mediates tau-induced neurotoxicity by calpain and ERK/MAPK activation.
    Authors: Amadoro Et al.
    Proc Natl Acad Sci U S A 2006;103:2892

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