| Description | GSK 650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor. |
| 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[4]. 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[5]. |
| Cell experiments | LNCaP cells are plated at a density of 5,000 cells per well in 96-well plates in 100 μL PRF-RPMI 1640, supplemented with 8% CS-FBS, 0.1 mM NEAA, and 1 mM NaPyr. At day three, cells are treated with hormone with or without GSK650394 by removing 50 μL of the media and replacing this with 50 μL of PRF-RPMI 1640 with 8% CS-FBS, NEAA, NaPyr containing a 2X concentration of the appropriate hormone/inhibitor treatment. At days 5 and 7, the treatment is repeated. On the tenth day, the media is removed and the relative cell number is measured using the FluoReporter Blue assay according to the manufacturer's instructions.(Only for Reference) |
| Target activity | SGK1:62 nM, SGK2:103 nM |
| Synonyms | GSK650394 |
| molecular weight | 382.45 |
| Molecular formula | C25H22N2O2 |
| CAS | 890842-28-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (130.74 mM) |
| References | 1. Sherk AB, et al. Cancer Res. 2008, 68(18), 7475-7483. 2. Anacker C, et al. Proc Natl Acad Sci U S A. 2013, 110(21), 8708-8713. 3. Alamares-Sapuay JG, et al. J Virol. 2013, 87(10), 6020-6066. 4. Peng HY, et al. Spinal SGK1/GRASP-1/Rab4 is involved in complete Freund's adjuvant-induced inflammatory pain via regulating dorsal horn GluR1-containing AMPA receptor trafficking in rats. Pain. 2012 Dec;153(12):2380-92. 5. Peng HY, et al. Spinal serum-inducible and glucocorticoid-inducible kinase 1 mediates neuropathic pain via kalirin and downstream PSD-95-dependent NR2B phosphorylation in rats. J Neurosci. 2013 Mar 20;33(12):5227-40. |