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Furin convertase inhibitor (chloromethylketone)

Highly specific, potent, irreversible, and cell-permeable competitive inhibitor of proprotein convertases.
 
ALX-260-022-M001 1 mg 165.00 USD
 
ALX-260-022-M005 5 mg 720.00 USD
Do you need bulk/larger quantities?
 
Replaces Prod. #: BML-PI132

Highly specific, potent, irreversible, and cell-permeable competitive inhibitor of proprotein convertases: furin/SPC1 (Ki~1nM), SPC2/PC2 (Ki=0.36nM), SPC3/PC1/PC3(Ki=2.0nM), SPC4/PACE4 (Ki=3.6nM), SPC6/PC5/PC6, and SPC7/LPC/PC7/PC8 (Ki=0.12nM). Because furin activates viral glycoproteins, this inhibitor is a useful antiviral agent. In addition, it inhibits furin-dependent pro-MMP-2 activation in various cell lines, including U87 and HT1080 cells. Typical concentration range used in tissue culture is 25-100µM.

Product Specification

Alternative Name:Decanoyl-Arg-Val-Lys-Arg-chloromethylketone, Dec-RVKR-CMK, TACE inhibitor
 
Formula:C34H66N11O5Cl . 3TFA
 
MW:744.3 . 342.1
 
Purity:≥95% (HPLC)
 
Appearance:White to off-white powder.
 
Solubility:Soluble in DMSO, methanol or water.
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
ALX-260-022 structure
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ALX-260-022 structure

Product Literature References

Artemisinins Target GABAA Receptor Signaling and Impair α Cell Identity: J. Li, et al.; Cell (2016), Abstract;
Enhancing dengue virus maturation using a stable furin over-expressing cell line: S. Mukherjee, et al.; Virology 497, 33 (2016), Application(s): Cell culture, reduce the efficiency of prM cleavage in virus preparations, Abstract;
Secreted factors from adipose tissue-derived mesenchymal stem cells suppress oxygen/glucose deprivation-induced cardiomyocyte cell death via furin/PCSK-like enzyme activity: Y. Tachida, et al.; Biochem. Biophys. Rep. (2016), Application(s): Furin/PCSK-like enzyme activity in synthetic substrate,
Secretome Signature Identifies ADAM17 as Novel Target for Radiosensitization of Non-Small Cell Lung Cancer: A. Sharma, et al.; Clin. Cancer. Res. 22, 4428 (2016), Application(s): Cell culture, Abstract; Full Text
Fluid shear stress promotes proprotein convertase-dependent activation of MT1-MMP: H. Kang, et al.; Biochem. Biophys. Res. Commun. 460, 596 (2015), Application(s): Cell Culture, Abstract;
PCSK6-mediated corin activation is essential for normal blood pressure: S. Chen, et al.; Nat. Med. 21, 1048 (2015), Application(s): Trypsin digestion, Abstract;
Enhanced UV-Induced Skin Carcinogenesis in Transgenic Mice Overexpressing Proprotein Convertases: J. Fu, et al.; Neoplasia 15, 169 (2013), Application(s): Western Blot, Abstract; Full Text
Proprotein Convertases Process and Thereby Inactivate Formylglycine-generating Enzyme: E. C. Ennemann, et al.; J. Biol. Chem. 288, 5828 (2013), Application(s): Cell Culture, Abstract; Full Text
Activation of the Epithelial Sodium Channel (ENaC) by the Alkaline Protease from Pseudomonas aeruginosa: M.B. Butterworth, et al.; J. Biol. Chem. 287, 32556 (2012), Application(s): Cell Culture, Abstract; Full Text
Decorin is Processed by Three Isoforms of Bone Morphogenetic Protein-1 (BMP1): Z. Von Marschall, et al.; Biochem. Biophys. Res. Commun. 391, 1374 (2010), Application(s): Cell Culture, Abstract; Full Text
Inhibitory potency and specificity of subtilase-like pro-protein convertase (SPC) prodomains: M. Fugere, et al.; J. Biol. Chem. 277, 7648 (2002), Abstract;
Shedding of the Transferrin Receptor Is Mediated Constitutively by an Integral Membrane Metalloprotease Sensitive to Tumor Necrosis Factor alpha Protease Inhibitor-2: M. Kaup, et al.; J. Biol. Chem. 277, 38494 (2002), Abstract; Full Text
Activated isoforms of MMP-2 are induced in U87 human glioma cells in response to beta-amyloid peptide: S. Deb, et al.; J. Neurosci. Res. 55, 44 (1999), Abstract;
Furin-independent pathway of membrane type 1-matrix metalloproteinase activation in rabbit dermal fibroblasts: T. Sato; J. Biol. Chem. 274, 37280 (1999), Abstract;
alpha1-Antitrypsin Portland, a bioengineered serpin highly selective for furin: application as an antipathogenic agent: F. Jean, et al.; PNAS 95, 7293 (1998), Abstract;
Inhibition of matrix metalloproteinase 2 maturation and HT1080 invasiveness by a synthetic furin inhibitor: E. Maquoi, et al.; FEBS Lett. 424, 262 (1998), Abstract;
PACE4: a subtilisin-like endoprotease with unique properties: R.E. Mains, et al.; Biochem. J. 321, 587 (1997), Abstract;
Inhibition of convertase-related processing of proendothelin-1: J.B. Denault, et al.; J. Cardiovasc. Pharmacol. 26 Suppl 3, S47 (1995), Abstract;
Processing of proendothelin-1 by human furin convertase: J.B. Denault, et al.; FEBS Lett. 362, 276 (1995), Abstract;
Proteolytic processing of human cytomegalovirus glycoprotein B (gpUL55) is mediated by the human endoprotease furin: M. Vey, et al.; Virology 206, 746 (1995), Abstract;
Processing of viral glycoproteins by the subtilisin-like endoprotease furin and its inhibition by specific peptidylchloroalkylketones: W. Garten, et al.; Biochimie 76, 217 (1994), Abstract;
The synthesis of inhibitors for processing proteinases and their action on the Kex2 proteinase of yeast: H. Angliker, et al.; Biochem. J. 293, 75 (1993), Abstract;
Influenza virus hemagglutinin with multibasic cleavage site is activated by furin, a subtilisin-like endoprotease: A. Stienke-Grober, et al.; EMBO J. 11, 2407 (1992), Abstract;
Inhibition of proteolytic activation of influenza virus hemagglutinin by specific peptidyl chloroalkyl ketones: W. Garten, et al.; Virology 172, 25 (1989), Abstract;

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