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Merck
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Documentos clave

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.

Sinónimos:

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

Fórmula empírica (notación de Hill):
C35H55N15O4
Peso molecular:
749.91
Código UNSPSC:
12352200

Nivel de calidad

Ensayo

≥98% (HPLC)

Formulario

solid

potencia

16 pM Ki

fabricante / nombre comercial

Calbiochem®

condiciones de almacenamiento

OK to freeze
protect from light

color

white

solubilidad

DMSO: 100 mg/mL

Condiciones de envío

ambient

temp. de almacenamiento

−20°C

Descripción general

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.

Acciones bioquímicas o fisiológicas

Cell permeable: yes
Primary Target
Furin, PAEC4, PC1/3, PC4, and PC5/6
Reversible: yes

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Forma física

Supplied as a trifluoroacetate salt.

Reconstitución

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Otras notas

Becker, G., et al. 2012. J Biol Chem287, 21992.

Información legal

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 1

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable


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