Cas No.: | 342795-08-8 |
Chemical Name: | Bragsin2 |
Synonyms: | Bragsin2;STK838884;6-methoxy-5-nitro-2-trifluoromethylchromone;6-methoxy-5-nitro-2-(trifluoromethyl)-4H-chromen-4-one |
SMILES: | FC(C1=C([H])C(C2C(=C(C([H])=C([H])C=2O1)OC([H])([H])[H])[N+](=O)[O-])=O)(F)F |
Formula: | C11H6F3NO5 |
M.Wt: | 289.1643 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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]. |
In Vitro: | 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]. |
References: | [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. |