GSK 650394

GSK 650394CAS号: 890842-28-1分子式: C25H22N2O2分子量: 382.45描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
GSK 650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2, respectively.
纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
GSK-650394;GSK650394
外观
white to beige powder
可溶性/溶解性
DMSO : ≥ 40.7 mg/mL (106.42 mM)
生物活性
靶点
SGK1;SGK2
In vitro(体外研究)
GSK650394 inhibits SGK1-mediated epithelial transport with an IC50 of 0.6 μM in the SCC assay. In LNCaP cells, GSK650394 inhibits the androgen-mediated enhancement of Nedd4-2 phosphorylation and androgen-mediated cell growth. GSK650394 counteracts the Cortisol-induced decrease in neurogenesis, changes in Hedgehog signaling, and GR nuclear translocation. GSK 650394 inhibits replication of influenza virus by impairing the export of influenza vRNPs into the cytoplasm of A549 cells.
In vivo(体内研究)
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.

分子结构图

GSK 650394