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

BRAG2:3 μM

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].