GSK650394

Research use only, not for human use.

GSK650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor.

GSK650394 is a competitive inhibitor that quantitatively blocks the effect of androgens on LNCaP cell growth.

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.

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.

GSK650394 | GSK-650394 | GSK 650394

Cytoskeleton/Cell Adhesion Molecules

HSP

SGK1| SGK2

Cancer

——

890842-28-1

382.45

C25H22N2O2

>98% (HPLC)

DMSO : ≥ 40.7 mg/mL; 106.42 mM

OC(=O)c1c(cc(cc1)c1c[nH]c2ncc(cc12)c1ccccc1)C1CCCC1

2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid.

(-20℃)

With Ice Pack

≥ 2 years