362330

GAG Antagonist, Surfen

The GAG Antagonist, Surfen controls the biological activity of GAG. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

• Sinônimo(s): GAG Antagonist, Surfen, Gβγ Activator, 12155, NSC12155, bis-2-Methyl-4-amino-quinolyl-6-carbamide, diHCl, trihydrate, Glycosaminoglycans Antagonist
• Fórmula empírica (Notação de Hill): C₂₁H₂₀N₆O · 2HCl · 3H₂O
• Peso molecular: 499.39
• Código UNSPSC: 12352200

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥98% (HPLC)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; desiccated (hygroscopic); protect from light
• cor: white
• solubilidade: DMSO: 50 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 2-8°C

Descrição

Descrição geral

A symmetrical quinolyl-urea compound that binds GAGs (glycosaminoglycans) via electrostatic interaction with the negatively charged sulfate and carboxyl moieties present in heparan sulfate (HS), heparin, and dermatan sulfate, resulting in effective blockage of GAGs interactions with their protein binding partners. Surfen is shown to effectively neutralize HS- and heparin-mediated thrombin inhibition of Factor Xa activity as well as heparin′s anti-clotting activity. Also reported to inhibit FGF2-induced Erk phosphorylation and tubulation in murine lung endothelial cultures (IC₅₀ ~5 µM), fibronectin HS-binding domain-dependent CHO cell adhesion (IC₅₀ = 3 µM), and HSV-1 infection of glucosaminyl 3-O-sulfotransferase-3A-expressing CHO cells (complete inhibition at 5 µM). Surfen analogs with improved potency may serve as promising candidates as less toxic alternatives to Protamine (Cat. No. 539122) in clinical applications.Reported to directly bind Gβγ subunit in a reversible manner, displace Gα-GDP from Gβγ, and acutely activate Gβγ signaling without Gα activation.

A symmetrical quinolyl-urea compound that binds GAGs (glycosaminoglycans) via electrostatic interaction with the negatively charged sulfate and carboxyl moieties present in heparan sulfate (HS), heparin, and dermatan sulfate, resulting in effective blockage of GAGs interactions with their protein binding partners. Surfen is shown to effectively neutralize HS- and heparin-mediated thrombin inhibition of Factor Xa activity as well as heparin′s anti-clotting activity. Also reported to inhibit FGF2-induced Erk phosphorylation and tubulation in murine lung endothelial cultures (IC₅₀ ~5 µM), fibronectin HS-binding domain-dependent CHO cell adhesion (IC₅₀ = 3 µM), and HSV-1 infection of glucosaminyl 3-O-sulfotransferase-3A-expressing CHO cells (complete inhibition at 5 µM). Surfen analogs with improved potency may serve as promising candidates as less toxic alternatives to Protamine (Cat. No. 539122) in clinical applications.

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot into glass vials and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Outras notas

Surve, C.R., et al. 2016. Sci. Signal.9, ra22.
Schuksz, M., et al. 2008. Proc. Natl. Acad. Sci. USA105, 13074.
Hunter, D.T. Jr., and Hill, J.M. 1961. Nature191, 1378.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 1
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable