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
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About This Item
Fórmula empírica (Notação de Hill):
C21H20N6O · 2HCl · 3H2O
Peso molecular:
499.39
Código UNSPSC:
12352200
Preço e disponibilidade não estão disponíveis no momento.
Produtos recomendados
Nível de qualidade
Ensaio
≥98% (HPLC)
Formulário
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 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.
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.
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
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
Certificados de análise (COA)
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Safder S Ganaie et al.
Cell, 184(20), 5163-5178 (2021-09-25)
Rift Valley fever virus (RVFV) is a zoonotic pathogen with pandemic potential. RVFV entry is mediated by the viral glycoprotein (Gn), but host entry factors remain poorly defined. Our genome-wide CRISPR screen identified low-density lipoprotein receptor-related protein 1 (mouse Lrp1/human
Ferenc Zsila
Chirality, 27(9), 605-612 (2015-06-23)
Despite the diverse biological activities of the glycosaminoglycan (GAG) antagonist surfen, the molecular details of its interaction with biomacromolecules remain poorly understood. Therefore, heparin and DNA binding properties of surfen were studied by circular dichroism (CD) and UV absorption spectroscopy
Ferenc Zsila
Biochemical and biophysical research communications, 460(3), 863-867 (2015-04-02)
It is shown that the heparin antagonist bis-aminoquinoline derivative surfen interacts with sulfated cyclodextrins in a unique fashion. Analysis of the UV spectroscopic data revealed exceptionally strong association (K(a) ∼ 10(7) M(-1)) of several surfen molecules to the external surface
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