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 Details
| Alternative Name: | Decanoyl-Arg-Val-Lys-Arg-chloromethylketone, Dec-RVKR-CMK, TACE inhibitor |
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| Formula: | C34H66N11O5Cl . 3TFA |
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| MW: | 744.3 . 342.1 |
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| Purity: | ≥95% (HPLC) |
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| Appearance: | White to off-white powder. |
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| Solubility: | Soluble in DMSO, methanol or water. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
prM-reactive antibodies reveal a role for partially mature virions in dengue virus pathogenesis: K.A. Dowd, et al.; PNAS
120, e2218899120 (2023),
Abstract;
Molecular Mechanism for Antibody-Dependent Enhancement of Coronavirus Entry: Y. Wan, et al.; J. Virol.
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Application(s): Treatment of cell culture,
Abstract;
Full Text
Cleavage activates Dispatched for Sonic Hedgehog ligand release: D.P. Stewart, et al.; Elife
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Abstract;
Full Text
Artemisinins Target GABAA Receptor Signaling and Impair α Cell Identity: J. Li, et al.; Cell
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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;
Human IGF1 pro-forms induce breast cancer cell proliferation via the IGF1 receptor: M. de Santi, et al.; Cell. Oncol. (Dordr.)
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Application(s): Treatment of HEK293 cells,
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.
7, 266 (2016),
Application(s): Furin/PCSK-like enzyme activity in synthetic substrate,
Abstract;
Full Text
Secretome Signature Identifies ADAM17 as Novel Target for Radiosensitization of Non-Small Cell Lung Cancer: A. Sharma, et al.; Clin. Cancer. Res.
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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
In vitro and in vivo activation induces BAFF and APRIL expression in B cells: V.T. Chu, et al.; J. Immunol.
179, 5947 (2007),
Application(s): Cell culture of mouse B cells,
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.
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Abstract;
alpha1-Antitrypsin Portland, a bioengineered serpin highly selective for furin: application as an antipathogenic agent: F. Jean, et al.; PNAS
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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.
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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
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Abstract;
The synthesis of inhibitors for processing proteinases and their action on the Kex2 proteinase of yeast: H. Angliker, et al.; Biochem. J.
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Abstract;
Influenza virus hemagglutinin with multibasic cleavage site is activated by furin, a subtilisin-like endoprotease: A. Stienke-Grober, et al.; EMBO J.
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Abstract;
Inhibition of proteolytic activation of influenza virus hemagglutinin by specific peptidyl chloroalkyl ketones: W. Garten, et al.; Virology
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Abstract;
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