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GSK 650394

Catalog No. T2622 CAS 890842-28-1

Synonyms: GSK650394

GSK 650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

GSK 650394, CAS 890842-28-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 48.00
5 mg	In stock	$ 80.00
10 mg	In stock	$ 113.00
25 mg	In stock	$ 219.00
50 mg	In stock	$ 396.00
100 mg	In stock	$ 568.00
200 mg	In stock	$ 698.00
1 mL * 10 mM (in DMSO)	In stock	$ 89.00

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Purity: 100%

Purity: 98.93%

Purity: 98.34%

Purity: 97.98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GSK 650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor.
Targets&IC50	SGK2:103 nM, SGK1:62 nM
In vivo	GSK650394, administered intrathecally in dosages of 1, 10, and 30 μM (10 μL/rat), effectively mitigates CFA-induced pain behaviors by inhibiting SGK1 phosphorylation, GluR1 trafficking, and protein-protein interactions, demonstrating its effects in a dose-dependent manner one day post-CFA administration. Additionally, this compound, at concentrations of 10, 30, and 100 nM (10 μL), significantly enhances the withdrawal latency of the ipsilateral hindpaw in a dose-dependent fashion, contrasting with the ineffective vehicle solution. This enhancement occurs 1-3 and 1-5 hours following injection, on days 3 and 7 post-surgery, respectively. From day 0 to day 6 post-surgery, GSK650394 (100 nM, 10 μL) alleviates SNL-induced allodynia on days 3, 5, and 7 in SNL subjects, suggesting its potent role in pain management through various mechanisms.
Kinase Assay	Scintillation proximity assay (SPA): SGK1 S422D (60–431 aa; 0.275 μg/mL final concentration) or SGK2 (0.875 μg/mL final concentration) are activated by PDK1 (1.1 μg/mL final concentration) in a buffer consisting of 50 mM Tris (pH 7.5), 0.1 mM EGTA, 0.1 mM EDTA, 10 mM MgCl2, 0.1% β-mercaptoethanol, 1 mg/mL BSA, and ATP (final concentration of 0.15 mM) and incubated for 30 min at 30°C. SGK2 is prepared exactly as described for SGK1, except it corresponded to the full-length protein. A solution containing biotinylated CROSStide peptide at a final concentration of 75 μM and γ32P-ATP corresponding to 2×106 cpm is prepared in the reaction buffer. In a 96-well plate, 5 μL of GSK650394 is added to 25 μL of the activated enzyme mixture. To this, 20 μL of the CROSStide mixture is added and incubated for 1 h at room temperature. Next, 50 μL of a 25 mg/mL slurry of streptavidin-coated SPA beads in PBS with 0.1 M EDTA, pH 8.0 is added. The plate is then sealed and centrifuged for 8 min at 2000 rpm, and the signal is detected by measuring for 30 sec/well in a Packard TopCount NXT Scintillation Counter. The IC50 values of the inhibition of SGK1 and SGK2 activities by GSK650394 are calculated from these data using GraphPad Prism 3 Software.
Cell Research	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)

Synonyms	GSK650394
Molecular Weight	382.45
Formula	C25H22N2O2
CAS No.	890842-28-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 38.2 mg/mL (100 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Infection Compound Library Bioactive Compounds Library Max Bioactive Compound Library Anti-Viral Compound Library Anti-Metabolism Disease Compound Library Metabolism Compound Library Kinase Inhibitor Library NO PAINS Compound Library Glycometabolism Compound Library

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Keywords

GSK 650394 890842-28-1 Metabolism Microbiology/Virology Influenza Virus SGK inhibit Serum-glucocorticoid regulated kinase Inhibitor GSK650394 Serum and glucocorticoid-regulated kinase GSK-650394 inhibitor

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