| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 3 μM (BRAG2) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | Bragsin2 | ||||||||||||
| CAS | 342795-08-8 | ||||||||||||
| Formula | C11H6F3NO5 | ||||||||||||
| Molar Mass | 289.16 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |