GSK650394 is a serum - and glucocorticoid-regulated kinase 1 inhibitor with an IC50 of 62 nM and 103 nM against SGK1 and SGK2, respectively.

 

Brand: BCM

 

Target: SGK; Influenza Virus

 

Signaling Pathways: Metabolism; Microbiology/Virology

 

In Vitro: GSK650394 inhibited SGK1-mediated epithelial cell transport with an IC50 of 0.6 μM in the SCC assay. In LNCaP cells, GSK650394 inhibited the androgen-mediated increase in Nedd4-2 phosphorylation and androgen-mediated cell growth. GSK650394 counteracts cortisol-induced reduction in nerve regeneration, altered Hedgehog signaling, and GR nuclear trafficking. GSK 650394 inhibited influenza virus replication by attenuating the transport of influenza vRNPs to the cytoplasm of A549 cells.

 

In Vivo: GSK650394 (1, 10, and 30 μM, 10 μL/rat, intrathecally) prevents CFA-induced pain behavior and the associates SGK1 phosphorylation, GluR1 trafficking, and protein-protein interactions at 1 day after CFA administration in a dose-dependent manner. 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.

 

Solubility: Soluble in DMSO. Insoluble in Water; Insoluble in Ethanol.

 

Isomeric SMILES: C1CCC(C1)C2=C(C=CC(=C2)C3=CNC4=C3C=C(C=N4)C5=CC=CC=C5)C(=O)O  

 

InChIKey: WVSBGSNVCDAMCF-UHFFFAOYSA-N  

 

InChI: InChI=1S/C25H22N2O2/c28-25(29)20-11-10-18(12-21(20)17-8-4-5-9-17)23-15-27-24-22(23)13-19(14-26-24)16-6-2-1-3-7-16/h1-3,6-7,10-15,17H,4-5,8-9H2,(H,26,27)(H,28,29)

 

Attribute
[CAS No.]	890842-28-1
[Formula]	C25H22N2O2
[Molecular]	382.5
[Chem Name]	2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid
[Storage]	Sealed in dry. Room Temperature
[Synonym]	GSK650394
[MDL No.]	MFCD12828779
[Form]	White to beige powder

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