Chemical Name: N-Benzyloxycarbonyl-L-leucylnorleucinal
Biological ActivityCalpeptin 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.
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Cell-penetrating inhibitors of calpain.
Inhibitory effect of di-and tripeptidyl aldehydes on calpains and cathepsins.
Sasaki et al.
J.Enzyme Inhib., 1990;3:195
Evidence for a calpeptin-sensitive protein-tyrosine phosphatase upstream of the small GTPase Rho.
Schoenwaelder and Burridge
Synthesis of a new cell penetrating calpain inhibitor (calpeptin).
Tsujinaka et al.
Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main protease.
Ma et al.
Cell Res., 2020;
Citations for Calpeptin
The citations listed below are publications that use Tocris products. Selected citations for Calpeptin include:
10 Citations: Showing 1 - 10
Calpeptin Reduces Neurobehavioral Deficits and Neuronal Apoptosis Following Subarachnoid Hemorrhage in Rats.
Authors: Zhou and Cai
J Stroke Cerebrovasc Dis 2019;28:125
Involvement of calpains in adult neurogenesis: implications for stroke.
Authors: Machado Et al.
J Biol Chem 2015;9:22
MFN2 couples glutamate excitotoxicity and mitochondrial dysfunction in motor neurons.
Authors: Wang Et al.
J Pharmacol Exp Ther 2015;290:168
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
Platelet surface-associated activation and secretion-mediated inhibition of coagulation factor XII.
Authors: Zakharova Et al.
PLoS One 2015;10:e0116665
Calpain cleavage within dysferlin exon 40a releases a synaptotagmin-like module for membrane repair.
Authors: Redpath Et al.
Mol Biol Cell 2014;25:3037
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
Distinct regulatory functions of calpain 1 and 2 during neural stem cell self-renewal and differentiation.
Authors: Santos Et al.
PLoS One 2012;7:e33468
Mitochondrial control of platelet apoptosis: effect of cyclosporin A, an inhibitor of the mitochondrial permeability transition pore.
Authors: Leytin Et al.
Lab Invest 2009;89:374
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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