Bragsin2 是非竞争性的核苷酸交换因子BRAG2选择性抑制剂，其IC50值为 3 μM。它能够结合到 BRAG2 的 PH 结构域和磷脂双分子层的界面处，使 BRAG2 无法激活磷脂化的 Arf GTPase。它能够影响乳腺癌干细胞。

Bragsin2 is a hydration-resistant cell penetrant, selective and non-competitive inhibitor of Afr guanine nucleotide exchange factor BRAG2 that inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin2 binds at the interface between the pleckstrin homology domain of BRAG2 and the lipid bilayer, leading BRAG2 unable to activate lipidated Arf GTPase.

Administration of 50?μM Bragsin2 inhibits Arf GTPase activation in HeLa cells[1]. Administration of 50?μM Bragsin2 inhibits the growth of breast cancer stem cells including SUM149 and S68, but has no effect on SUM159, which lacks adhesion molecules such as integrin and cadherin[1].

342795-08-8

C11H6F3NO5

289.16

6-methoxy-5-nitro-2-(trifluoromethyl)chromen-4-one;Bragsin 2;Bragsin2

DMSO:55 mg/ml (190.21 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years