Decanoyl-RVKR-CMK

Catalog #: 3501
13 Citations Datasheet / COA / SDS

Catalog #	Availability	Size / Price	Qty
3501/1

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Description: Subtilisin/Kex2p-like proprotein convertase inhibitor

Purity: ≥95%

View All Products for Furin Inhibitors

Product Details

Citations (13)

Reviews

Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

Decanoyl-RVKR-CMK is a 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. Inhibits cleavage of glycoprotein B of human cytomegalovirus. Also inhibits cleavage of SARS-CoV-2 spike protein by furin and blocks viral cell entry (IC₅₀ = 57 nM in plaque reduction assay).

Technical Data

M.Wt:

744.42

Formula:

C₃₄H₆₆ClN₁₁O₅

Sequence:

RVKR

(Modifications: Arg-1 = Decanoyl-Arg, Arg-4 = chlororomethylketone)

Solubility:

Soluble to 1 mg/ml in water

Purity:

≥95%

Storage:

Store at -20°C

CAS No:

150113-99-8

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.

Background References

A prohormone convertase cleavage site within a predicted alpha-helix mediates sorting of the neuronal and endocrine polypeptide VGF into the regulated secretory pathway.
Garcia et al.
J.Biol.Chem., 2005;280:41595
Comparative study of the binding pocket of mammalian proprotein convertases and its implications for the design of specific small molecule inhibitors.
Tian and Jianhua
Int.J.Biol.Sci., 2010;6:89
Inhibition of convertase-related processing of proendothelin-1.
Denault et al.
J.Cardiovasc.Pharmacol., 1995;26:S47
Furin inhibitors block SARS-CoV-2 spike protein cleavage to suppress virus production and cytopathic effects.
Cheng et al.
Cell Rep., 2020;

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Citations for Decanoyl-RVKR-CMK

The citations listed below are publications that use Tocris products. Selected citations for Decanoyl-RVKR-CMK include:

13 Citations: Showing 1 - 10

A bat MERS-like coronavirus circulates in pangolins and utilizes human DPP4 and host proteases for cell entry.
Authors: Wei Et al.
Cell 2023;186:850-863.e16
High-throughput measurement of the content and properties of nano-sized bioparticles with single-particle profiler.
Authors: Jurga Et al.
Nat Biotechnol 2023;
A Newly Engineered A549 Cell Line Expressing ACE2 and TMPRSS2 Is Highly Permissive to SARS-CoV-2, Including the Delta and Omicron Variants.
Authors: Robert W Et al.
Viruses 2022;14
Host and viral determinants for efficient SARS-CoV-2 infection of the human lung.
Authors: Dong Et al.
Nat Commun 2021;12:134
SARS-CoV-2 requires cholesterol for viral entry and pathological syncytia formation.
Authors: Robert F Et al.
Elife 2021;10
The half-life of the bone-derived hormone osteocalcin is regulated through O-glycosylation in mice, but not in humans.
Authors: Henrik Et al.
Elife 2020;9
A Multibasic Cleavage Site in the Spike Protein of SARS-CoV-2 Is Essential for Infection of Human Lung Cells.
Authors: Hoffman Et al.
Mol Cell 2020;78:779
Furin inhibitors block SARS-CoV-2 spike protein cleavage to suppress virus production and cytopathic effects.
Authors: Cheng Et al.
Cell Rep. 2020;33:108254
Biowire Model of Interstitial and Focal Cardiac Fibrosis.
Authors: Wang Et al.
ACS Cent Sci 2019;5:1146
Middle East Respiratory Syndrome Coronavirus Spike Protein Is Not Activated Directly by Cellular Furin during Viral Entry into Target Cells.
Authors: Matsuyama Et al.
J Virol 2018;92

Cutting Edge: ERK1 Mediates the Autocrine Positive Feedback Loop of TGF-β and Furin in Glioma-Initiating Cells.
Authors: Michael Et al.
J Immunol 2017;198:4569-4574

The role of interleukin-13 in the removal of hyper-radiosensitivity by priming irradiation.
Authors: Edin
Am J Physiol Gastrointest Liver Physiol 2014;55:1066

Host cell entry of Middle East respiratory syndrome coronavirus after two-step, furin-mediated activation of the spike protein.
Authors: Millet & Whittaker
Proc Natl Acad Sci U S A 2014;111:15214

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