GSK 650394

• CAT Number: I005336
• CAS Number: 890842-28-1
• Molecular Formula: C25H22N2O2
• Molecular Weight: 382.5
• Purity: ≥95%
• Target: SGK
• Solubility: DMSO: ≥ 40.7 mg/mL
• Storage: Store at -20C
• IC50: 62 nM (SGK1); 103 nM (SGK2) [1]
• 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)
• InChIKey: WVSBGSNVCDAMCF-UHFFFAOYSA-N
• SMILES: O=C(O)C(C(C1CCCC1)=C2)=CC=C2C3=CNC4=NC=C(C5=CC=CC=C5)C=C43

GSK650394（Cat No.:I005336） is a newly developed SGK inhibitor exhibiting potent activity against SGK1 and SGK2, as determined by the SPA assay. With an IC50 value of 62 nM for SGK1 and 103 nM for SGK2, it demonstrates strong inhibitory effects on both isoforms. This novel compound shows promise for further exploration and development in the field of SGK inhibition.

Reference

[1]. Sherk AB, et al. Development of a small-molecule serum- and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic. Cancer Res. 2008 Sep 15;68(18):7475-83.
[2]. Mansley MK, et al. Effects of nominally selective inhibitors of the kinases PI3K, SGK1 and PKB on the insulin-dependent control of epithelial Na+ absorption. Br J Pharmacol. 2010 Oct;161(3):571-88.
[3]. 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.
[4]. 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.