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说明： Calpain and cathepsin L inhibitor
化学名： N-Benzyloxycarbonyl-L-leucylnorleucinal
生物活性 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.
技术数据 for Calpeptin
| 分子量 | 362.47 |
| 公式 | C20H30N2O4 |
| 储存 | 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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for Calpeptin
参考文献 for Calpeptin
参考文献是支持产品生物活性的出版物。
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
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关键词: 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 篇 Calpeptin 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Calpeptin 的部分引用包括：
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
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
Zhou and Cai (2019) Calpeptin Reduces Neurobehavioral Deficits and Neuronal Apoptosis Following Subarachnoid Hemorrhage in Rats. J Stroke Cerebrovasc Dis 28 125 PMID: 30337208
Zakharova et al (2015) Platelet surface-associated activation and secretion-mediated inhibition of coagulation factor XII. PLoS One 10 e0116665 PMID: 25688860
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
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
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
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