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.