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.

• 別名: GAG Antagonist, Surfen, Gβγ Activator, 12155, NSC12155, bis-2-Methyl-4-amino-quinolyl-6-carbamide, diHCl, trihydrate, Glycosaminoglycans Antagonist
• 実験式（ヒル表記法）: C₂₁H₂₀N₆O · 2HCl · 3H₂O
• 分子量: 499.39
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated (hygroscopic); protect from light
• 色: white
• 溶解性: DMSO: 50 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C

詳細

詳細

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.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 1
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable