Bragsin1 是一种有效、选择性、非竞争性的核苷酸交换因子 ArfGEF BRAG2 抑制剂，抑制 Arf GTPase 活化，IC50 值为 3 μM。Bragsin1 与 BRAG2 的 PH 结构域结合，为非竞争性界面抑制剂，对人 ArfGEFs 的 Sec7 结构域无作用。具有抗肿瘤活性。
| Cas No. | 369631-68-5 |
| 分子式 | C11H6F3NO4 |
| 分子量 | 273.16 |
| 溶解度 | DMSO : 62.5 mg/mL (228.80 mM; Need ultrasonic) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity[1]. [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. |
