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Subtilisin/Kex2p-like proprotein convertase inhibitor; blocks activity of all seven convertases (PC1, PC2, PC4, PACE4, PC5, PC7 and furin). Abolishes proET-1 processing in endothelial cells; inhibits regulated secretion of the neuronal polypeptide VGF in PC12 cells. Also inhibits cleavage of SARS-CoV-2 spike protein by furin and blocks viral cell entry (IC50 = 57 nM in plaque reduction assay).
(Modifications: Arg-1 = Decanoyl-Arg, Arg-4 = chlororomethylketone)
|Storage||Store at -20°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||Soluble to 1 mg/ml in water|
References are publications that support the biological activity of the product.
Garcia et al (2005) A prohormone convertase cleavage site within a predicted alpha-helix mediates sorting of the neuronal and endocrine polypeptide VGF into the regulated secretory pathway. J.Biol.Chem. 280 41595 PMID: 16221685
Tian and Jianhua (2010) Comparative study of the binding pocket of mammalian proprotein convertases and its implications for the design of specific small molecule inhibitors. Int.J.Biol.Sci. 6 89 PMID: 20151049
Denault et al (1995) Inhibition of convertase-related processing of proendothelin-1. J.Cardiovasc.Pharmacol. 26 S47 PMID: 8587448
Cheng et al (2020) Furin inhibitors block SARS-CoV-2 spike protein cleavage to suppress virus production and cytopathic effects. Cell Rep.
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Keywords: Decanoyl-RVKR-CMK, Decanoyl-RVKR-CMK supplier, proprotein, convertases, inhibitors, inhibits, supplier, proteolytic, cleavage, calcium, dependent, serine, endopeptidases, furin, PC1, PC2, PC4, PACE4, PC5, PC7, secretory, pathway, MERS, SARS, Other, Proteases, Furin, 3501, Tocris Bioscience
6 Citations for Decanoyl-RVKR-CMK
Citations are publications that use Tocris products. Selected citations for Decanoyl-RVKR-CMK include:
Hoffman et al (2020) A Multibasic Cleavage Site in the Spike Protein of SARS-CoV-2 Is Essential for Infection of Human Lung Cells. Mol Cell 78 779 PMID: 32362314
Cheng et al (2020) Furin inhibitors block SARS-CoV-2 spike protein cleavage to suppress virus production and cytopathic effects. Cell Rep. PMID: 33007239
Matsuyama et al (2018) Middle East Respiratory Syndrome Coronavirus Spike Protein Is Not Activated Directly by Cellular Furin during Viral Entry into Target Cells. J Virol 92 PMID: 30021905
Wang et al (2019) Biowire Model of Interstitial and Focal Cardiac Fibrosis. ACS Cent Sci 5 1146 PMID: 31403068
Millet & Whittaker (2014) Host cell entry of Middle East respiratory syndrome coronavirus after two-step, furin-mediated activation of the spike protein. Proc Natl Acad Sci U S A 111 15214 PMID: 25288733
Edin (2014) The role of interleukin-13 in the removal of hyper-radiosensitivity by priming irradiation. Am J Physiol Gastrointest Liver Physiol 55 1066 PMID: 24966400
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