342795-08-8

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 is a hydration resistant cell penetrantpotent and selective noncompetitive inhibitor of ArfGEF BRAG2 (Afr guanine nucleotide exchange factor BRAG2) th at inhibits Arf GTPase activation in vitro and in cells. It binds to pleckstrin homology (PH) domain of BRAG2 and misposition BRAG2 on the membrane. Bragsin2 disrupt the function of the yeast ArfGEF Sec7p. Bragsin2 suppresses tumorsphere formation of some breast cancer stem cell lines including SUM149 and S68.

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[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. DOI:10.1038/s41589-019-0228-3