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GSK 650394

CAS No. : 890842-28-1

MCE 国际站：GSK 650394

产品活性：GSK 650394 是一种新颖的 SGK 抑制剂，在SPA实验中，对 SGK1 和 SGK2 的IC₅₀ 分别为 62 nM 和 103 nM。GSK 650394 还可抑制流感病毒复制。

研究领域：Metabolic Enzyme/Protease  |  Anti-infection

作用靶点：SGK  |  Influenza Virus

In Vitro: GSK650394 is relatively non-toxic, with LC₅₀ values of 41 μM in M1 cells (68 times its activity IC₅₀) and a LC₅₀ greater than 100 μM in HeLa cells. GSK650394 inhibits SGK1-mediated epithelial transport with an IC₅₀ of 0.6 μM in the SCC assay. GSK650394 inhibits the growth of LNCaP cells with IC₅₀ of approximately 1 μM. GSK650394A inhibits the insulin-induced phosphorylation of PKB-Ser⁴⁷³ at 3 µM, and essentially abolishes this response at 10 µM. GSK650394A (1-10 µM) does not alter the phosphorylation of PRAS40-Ser246 in hormone-deprived cells or prevent the insulin-induced phosphorylation of this residue.

In Vivo: 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.

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