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537076

Sigma-Aldrich

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

100

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
Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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