For research use only. Not for therapeutic Use.
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].
| Catalog Number | I019504 |
| CAS Number | 342795-08-8 |
| Synonyms | 6-methoxy-5-nitro-2-(trifluoromethyl)chromen-4-one |
| Molecular Formula | C11H6F3NO5 |
| Purity | ≥95% |
| InChI | InChI=1S/C11H6F3NO5/c1-19-7-3-2-6-9(10(7)15(17)18)5(16)4-8(20-6)11(12,13)14/h2-4H,1H3 |
| InChIKey | WJUILHMXVGFAIS-UHFFFAOYSA-N |
| SMILES | COC1=C(C2=C(C=C1)OC(=CC2=O)C(F)(F)F)[N+](=O)[O-] |
| 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. |
