362330
GAG拮抗剂，Surfen
The GAG Antagonist, Surfen controls the biological activity of GAG. This small molecule/inhibitor is primarily used for Activators/Inducers applications.
别名:
GAG拮抗剂，Surfen, Gβγ活化剂，12155，NSC12155，双-2-甲基-4-氨基-喹啉基-6-脲，二盐酸盐，三水合物，糖胺聚糖拮抗剂
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
Quality Level
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
white
solubility
DMSO: 50 mg/mL
shipped in
ambient
General description
一种对称的喹啉基脲化合物，通过静电交互效应将GAG（糖胺聚糖）与硫酸乙酰肝素（HS）、肝素和硫酸皮肤素中存在的带负电荷的硫酸盐和羧基部分结合，从而通过其蛋白结合伴侣有效阻断GAG各种相互作用。已证明Surfen可有效中和HS和肝素介导的凝血酶对因子Xa活性以及肝素′抗凝活性的抑制作用。还报道了抑制FGF2诱导的鼠肺内皮培养物中的Erk磷酸化和输卵管形成（IC50 ~5 µM），纤维连接蛋白HS结合域依赖性CHO细胞粘连（IC50 = 3 µM）和表达葡萄胺基3-O-磺基转移酶-3A的CHO细胞的HSV-1感染（在5 µM时完全抑制）。具有改善的效价的Surfen类似物可以作为有希望的候选物，作为临床应用中鱼精蛋白（目录号539122）的毒性较小的替代品。据报道，它们以可逆的方式直接结合Gβγ亚基，从Gβγ取代Gα-GDP，并在没有Gα激活的情况下急性激活Gβγ信号传导。
Packaging
用惰性气体包装
Preparation Note
复溶后，等分至玻璃瓶中，并冷冻保存（-20°C）。储备溶液在-20°C下可稳定保存至多6个月。
Other Notes
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
毒性：标准处理（A）
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
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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