中文名称:

2-环戊基-4-(5-苯基-1H-吡咯并[2,3-B]吡啶-3-基)苯甲酸

中文同义词:

2-环戊基-4-(5-苯基-1H-吡咯并[2,3-B]吡啶-3-基)苯甲酸;SGK抑制剂(GSK 650394)

英文名称:

2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-benzoicacid

英文同义词:

GSK650394 (Free base);2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-benzoicacid;GSK 650394;SGK inhibitor GS650394;CS-1142;Benzoic acid, 2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-

CAS号:

890842-28-1

分子式:

C25H22N2O2

分子量:

382.45

EINECS号:

相关类别:

细胞生物学试剂;抑制剂;小分子抑制剂;小分子抑制剂，天然产物;Inhibitors

Mol文件:

890842-28-1.mol

储存条件 

room temp

溶解度 

DMSO: soluble20mg/mL, clear

形态

powder

颜色

white to beige

生物活性

GSK650394是一种血清和糖皮质激素调节的激酶-1抑制剂,对SGK1和SGK2的 IC50分别为62 nM和103 nM。

靶点

Target Value SGK1 (Cell-free assay) 62 nM SGK2 (Cell-free assay) 103 nM

Target

Value

SGK1 (Cell-free assay)

62 nM

SGK2 (Cell-free assay)

103 nM

体外研究

GSK650394抑制SGK1介导的上皮细胞转运，在SCC试验中IC50为0.6 μM。在LNCaP细胞中，GSK650394抑制雄激素介导的Nedd4-2磷酸化增加和雄激素介导的细胞生长。 GSK650394抵消皮质醇诱导的神经再生的减少，Hedgehog信号通路的改变，和GR核转运。GSK 650394通过减弱流感vRNPs转运到A549细胞的细胞质抑制流感病毒的复制。

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.

WGK Germany 

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