生物活性 GSK 650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively. GSK 650394 also inhibits influenza virus replication.
IC50 & Target SGK1
体外研究(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[1]. 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[2].
体内研究(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[3]. 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[4].
分子量 382.45
性状 Solid
Formula C25H22N2O2
CAS 号 890842-28-1
运输条件 Room temperature in continental US; may vary elsewhere.
储存方式 Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month 溶解性数据 In Vitro: DMSO : ≥ 40.7 mg/mL (106.42 mM)
* "≥" means soluble, but saturation unknown.
配制储备液 浓度溶剂体积质量 1 mg 5 mg 10 mg 1 mM 2.6147 mL 13.0736 mL 26.1472 mL 5 mM 0.5229 mL 2.6147 mL 5.2294 mL 10 mM 0.2615 mL 1.3074 mL 2.6147 mL * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: