537076
Proprotein Convertase Inhibitor
The Proprotein Convertase Inhibitor controls the biological activity of Proprotein Convertase. This small molecule/inhibitor is primarily used for Cell Signaling applications.
Synonym(s):
Proprotein Convertase Inhibitor, PACE4 Inhibitor, Furin-like Proprotein Convertase Inhibitor, Furin Inhibitor III, PC1/3 Inhibitor, PC4 Inhibitor, PC5/6 Inhibitor
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About This Item
Empirical Formula (Hill Notation):
C35H55N15O4
Molecular Weight:
749.91
UNSPSC Code:
12352200
Quality Level
Assay
≥98% (HPLC)
form
solid
potency
16 pM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white
solubility
DMSO: 100 mg/mL
shipped in
ambient
storage temp.
−20°C
General description
A cell-permeable tripeptide derivative containing an Arg-X-Arg motive that acts as a highly potent and reversible furin inhibitor (Ki = 16 pM). Also shown to inhibit several other pro-protein convertases, such as PC1/3, PC4, PAEC4, PC5/6 with almost similar potency, but does not affect PC2, PC7, and trypsin-like serine proteases in any significant manner. Acts as a very weak inhibitor of plasmin (Ki = 7.3 µM). Exhibits greater stability in cells. Shown to block hemagglutinin cleavage (40% at 1 µM) and fowl plague virus (FPV) viral propagation in a dose-dependent manner. Exhibits minimal toxicity even at high concentrations (25-50 µM) and protects human epidermoid carcinoma (HEp-2) cells from toxic effects of Shiga toxin.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Furin, PAEC4, PC1/3, PC4, and PC5/6
Furin, PAEC4, PC1/3, PC4, and PC5/6
Reversible: yes
Packaging
Packaged under inert gas
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Becker, G., et al. 2012. J Biol Chem287, 21992.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class Code
11 - Combustible Solids
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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