890842-28-1
890842-28-1 結(jié)構(gòu)式
基本信息
2-環(huán)戊基-4-(5-苯基-1H-吡咯并[2,3-B]吡啶-3-基)苯甲酸
GSK 650394
GSK650394 (Free base)
SGK inhibitor GS650394
2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-benzoicacid
Benzoic acid, 2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-
常見問題列表
| Target | Value |
|
SGK1
(Cell-free assay) | 62 nM |
|
SGK2
(Cell-free assay) | 103 nM |
GSK650394抑制SGK1介導(dǎo)的上皮細(xì)胞轉(zhuǎn)運(yùn)，在SCC試驗(yàn)中IC50為0.6 μM。在LNCaP細(xì)胞中，GSK650394抑制雄激素介導(dǎo)的Nedd4-2磷酸化增加和雄激素介導(dǎo)的細(xì)胞生長(zhǎng)。 GSK650394抵消皮質(zhì)醇誘導(dǎo)的神經(jīng)再生的減少，Hedgehog信號(hào)通路的改變，和GR核轉(zhuǎn)運(yùn)。GSK 650394通過減弱流感vRNPs轉(zhuǎn)運(yùn)到A549細(xì)胞的細(xì)胞質(zhì)抑制流感病毒的復(fù)制。
GSK650394 (1, 10, and 30 μM, 10 μL/rat, intrathecally) dose-dependently prevents CFA-induced pain behavior and the associates SGK1 phosphorylation, GluR1 trafficking, and protein-protein interactions at 1 day after CFA administration. GSK650394 at concentrations of 10, 30, and 100 nM (10 μL), but not vehicle solution (SNL 3D+Veh and SNL 7D+Veh, respectively), dose-dependently increases the withdrawal latency of the ipsilateral hindpaw at 1-3 and 1-5 h after injection at days 3 and 7 postsurgery (SNL 3D+GSK and SNL 7D+GSK, respectively). GSK650394 (from day 0 to 6 postsurgery; 100 nM, 10 μL, i.t.) administration alleviates SNL-induced allodynia at days 3, 5, and 7 postsurgery in SNL animals.