| 中文名称 | GGTI-298 |
| 英文名称 | GGTI-298 |
| CAS号 | 180977-44-0 |
| 分子式 | C27H33N3O3S |
| 分子量 | 479.63 |
| EINECS号 | 604-604-1 |
| 熔点 | 99.5-100 °C |
| 沸点 | 673.7±55.0 °C(Predicted) |
| 密度 | 1.190±0.06 g/cm3(Predicted) |
| 溶解度 | 二甲基亚砜:22 mg/毫升 |
| 形态 | 固体 |
| 酸度系数(pKa) | 9.83±0.10(Predicted) |
| 颜色 | 米白色 |
| 危险品标志 | Xi |
| 危险类别码 | 36/37/38 |
| 安全说明 | 26-36 |
| WGK Germany | 3 |
IC50: 3 μM (Rap1A, in vivo), > 20 μM (Ha-Ras, in vivo)
Both RhoA inhibitor (GGTI298) and ROCK inhibitor (H1152) significantly reduce cAMP agonist-stimulated IK(ap), whereas the latter additionally reduces colocalization of KCNN4c with the apical membrane marker wheat germ agglutinin in T84WT cells. Knockdown of DR4 abolishes NF-κB activation, leading to sensitization of DR5-dependent apoptosis induced by the combination of GGTI298 and TRAIL. GGTI298/TRAIL activates NF-κB and inhibits Akt. knockdown of DR5, preventes GGTI298/TRAIL-induced IκBα and p-Akt reduction, suggesting that DR5 mediates reduction of IκBα and p-Akt induced by GGTI298/TRAIL. In contrast, DR4 knockdown further facilitates GGTI298/TRAIL-induced p-Akt reduction.
The vivo mouse ileal loop experiments show fluid accumulation is reduced in a dose-dependent manner by TRAM-34, GGTI298, or H1152 when injected together with cholera toxin into the loop.