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Merck
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Key Documents

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.

Synonyme(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

Formule empirique (notation de Hill):
C35H55N15O4
Poids moléculaire :
749.91
Code UNSPSC :
12352200

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

solid

Puissance

16 pM Ki

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
protect from light

Couleur

white

Solubilité

DMSO: 100 mg/mL

Conditions d'expédition

ambient

Température de stockage

−20°C

Description générale

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.

Actions biochimiques/physiologiques

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

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Forme physique

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.

Autres remarques

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

Informations légales

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

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 1

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

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Yi He et al.
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Cartilage degradation is a hallmark of osteoarthritis (OA). Aggrecan, a major proteoglycan of articular cartilage extracellular matrix (ECM), is degraded by ADAMTS-5 resulting in the release of ARGS-G2 fragments to synovial fluid and circulation. The aim was to quantify ARGS-G2
Belinda Yau et al.
Scientific reports, 9(1), 19466-19466 (2019-12-21)
A threonine-to-Isoleucine (Thr52Ile) mutation within the pro-domain of the Sorcs1 gene was positionally cloned as the gene underlying a quantitative trait locus that affects fasting insulin levels in mice. In humans, genome-wide association studies and linkage studies have shown that

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