Bragsin2 是一种有效、选择性、和非竞争性的核苷酸交换因子 BRAG2 抑制剂，IC50 值为 3 μM。Bragsin2 结合于 BRAG2 的 PH 结构域和磷脂双分子层的界面处，导致 BRAG2 无法激活磷脂化的 Arf GTPase。Bragsin2 能够影响乳腺癌干细胞。
货号:ajcx38596
CAS:342795-08-8
分子式:C11H6F3NO5
分子量：289.16
溶解度:DMSO : 100 mg/mL (345.83 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存： 现货

Background:

Bragsin2 is a potent, selective and noncompetitive nucleotide exchange factor BRAG2 inhibitor, with an IC50 of 3 μM. Bragsin2 binds at the interface between the PH domain of BRAG2 and the lipid bilayer, leads BRAG2 unable to activate lipidated Arf GTPase. Bragsin2 affects breast cancer stem cells[1].

Bragsin2 (50 μM) inhibits Arf GTPase activation in HeLa cells[1].Bragsin2 (50 μM) inhibits the growth of SUM149 and S68, with no effect on SUM159, which lacks adhesion molecules such as integrins and cadherins[1].

[1]. Nawrotek A, et al. PH-domain-binding inhibitors of nucleotide exchange factor BRAG2 disrupt Arf GTPase signaling. Nat Chem Biol. 2019 Feb 11. doi: 10.1038/s41589-019-0228-3.