890842-28-1

890842-28-1 - Names and Identifiers

Name	2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-benzoicacid
Synonyms	CS-1142 GSK 650394 GSK650394 (Free base) SGK inhibitor GS650394 6-O-α-D-Glucopyranosyl-D-glucose 2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-benzoicacid Benzoic acid, 2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-
CAS	890842-28-1

890842-28-1 - Physico-chemical Properties

Molecular Formula	C25H22N2O2
Molar Mass	382.45
Solubility	DMSO: soluble20mg/mL, clear
Appearance	powder
Color	white to beige
Storage Condition	room temp
Use	GSK 650394 is a novel SGK inhibitor. In SPA experiments, the IC50 for SGK1 and SGK2 is 62 nM and 103 nM respectively. GSK 650394 can also inhibit influenza virus replication.
Target	IC50: 62 nM (SGK1), 103 nM (SGK2)
In vitro study	GSK650394 inhibits 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 the reduction of cortisol-induced nerve regeneration, alteration of Hedgehog signaling pathway, and GR-nuclear translocation. GSK 650394 inhibit influenza virus replication by attenuating influenza vRNPs transport into the cytoplasm of A549 cells.
In vivo study	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.

890842-28-1 - Risk and Safety

WGK Germany

890842-28-1 - Reference

Reference

1: Su Y, Qadri SM, Cayabyab FS, Wu L, Liu L. Regulation of methylglyoxal-elicited leukocyte recruitment by endothelial SGK1/GSK3 signaling. Biochim Biophys Acta. 2014 Jul 5;1843(11):2481-2491. doi: 10.1016/j.bbamcr.2014.06.018. [Epub ahead of print] PubMed PMID: 25003317.
2: Zhang L, Liu J, Liu Y, Xu Y, Zhao X, Qian J, Sun B, Xing C. Fluvastatin inhibits the expression of fibronectin in human peritoneal mesothelial cells induced by high-glucose peritoneal dialysis solution via SGK1 pathway. Clin Exp Nephrol. 2014 Jun 20. [Epub ahead of print] PubMed PMID: 24942605.
3: Mattes C, Laube M, Thome UH. Rapid elevation of sodium transport through insulin is mediated by AKT in alveolar cells. Physiol Rep. 2014 Mar 20;2(3):e00269. doi: 10.1002/phy2.269. Print 2014. PubMed PMID: 24760523; PubMed Central PMCID: PMC4002249.
4: Isikbay M, Otto K, Kregel S, Kach J, Cai Y, Vander Griend DJ, Conzen SD, Szmulewitz RZ. Glucocorticoid receptor activity contributes to resistance to androgen-targeted therapy in prostate cancer. Horm Cancer. 2014 Apr;5(2):72-89. doi: 10.1007/s12672-014-0173-2. Epub 2014 Mar 11. PubMed PMID: 24615402.
5: Chatterjee S, Schmidt S, Pouli S, Honisch S, Alkahtani S, Stournaras C, Lang F. Membrane androgen receptor sensitive Na+/H+ exchanger activity in prostate cancer cells. FEBS Lett. 2014 May 2;588(9):1571-9. doi: 10.1016/j.febslet.2014.02.040. Epub 2014 Mar 4. PubMed PMID: 24607544.
6: Bradford D, Raghuram V, Wilson JL, Chou CL, Hoffert JD, Knepper MA, Pisitkun T. Use of LC-M

890842-28-1 - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	2.615 ml	13.074 ml	26.147 ml
5 mM	0.523 ml	2.615 ml	5.229 ml
10 mM	0.261 ml	1.307 ml	2.615 ml
5 mM	0.052 ml	0.261 ml	0.523 ml

Last Update：2024-01-02 23:10:35

890842-28-1 - Cell Experiment

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) Cell lines: LNCaP cells

Last Update：2023-08-16 21:32:38