GSK 650394

Pricing Availability   Qty
Description: Serum- and glucocorticoid-regulated kinase (SGK) inhibitor
Chemical Name: 2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-benzoic acid
Purity: ≥97% (HPLC)
Citations (17)
Reviews (1)
Literature (2)

Biological Activity for GSK 650394

GSK 650394 is a serum- and glucocorticoid-regulated kinase 1 (SGK1) inhibitor (IC50 values are 62 and 103 nM for SGK1 and SGK2 respectively). Displays >30-fold selectivity over Akt and other related kinases. Inhibits androgen-stimulated growth of LNCaP cells, a human prostate carcinoma cell line (IC50 ~ 1 μM).

Licensing Information

Sold with the permission of GlaxoSmithKline

Compound Libraries for GSK 650394

GSK 650394 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for GSK 650394

M. Wt 382.45
Formula C25H22N2O2
Storage Store at RT
Purity ≥97% (HPLC)
CAS Number 890842-28-1
PubChem ID 25022668
Smiles O=C(C(C(C5CCCC5)=C4)=CC=C4C2=CNC1=NC=C(C3=CC=CC=C3)C=C12)O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for GSK 650394

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 38.24 100

Preparing Stock Solutions for GSK 650394

The following data is based on the product molecular weight 382.45. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.61 mL 13.07 mL 26.15 mL
5 mM 0.52 mL 2.61 mL 5.23 mL
10 mM 0.26 mL 1.31 mL 2.61 mL
50 mM 0.05 mL 0.26 mL 0.52 mL

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Product Datasheets for GSK 650394

Certificate of Analysis / Product Datasheet
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References for GSK 650394

References are publications that support the biological activity of the product.

Sherk et al (2008) Development of a small-molecule serum- and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic. Cancer Res. 68 7475 PMID: 18794135

Hall et al (2012) Serum and glucocorticoid-regulated kinase 1 (SGK1) activation in breast cancer: requirement for mTORC1 activity associates with ER-alpha expression. Breast Cancer Res.Treat 135 469 PMID: 22842983

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Keywords: GSK 650394, GSK 650394 supplier, Serum-, glucocorticoid-regulated, kinase, SGK1, inhibitors, inhibits, androgen, receptors, GSK650394, GlaxoSmithKline, GSK, Other, Kinases, Androgen, Receptor, 3572, Tocris Bioscience

17 Citations for GSK 650394

Citations are publications that use Tocris products. Selected citations for GSK 650394 include:

Matschke et al (2016) Role of SGK1 for fatty acid uptake, cell survival and radioresistance of NCI-H460 lung cancer cells exposed to acute or chronic cycling severe hypoxia. Radiat Oncol 11 75 PMID: 27251632

Juvekar et al (2016) Phosphoinositide 3-kinase inhibitors induce DNA damage through nucleoside depletion. Proc Natl Acad Sci U S A 113 E4338 PMID: 27402769

Messerschmidt et al (2019) Osmotic induction of cyclooxygenase-2 in RPE cells: Stimulation of inflammasome activation. Mol Vis 25 329 PMID: 31341381

Bossmann et al (2017) Signaling Cascade Involved in Rapid Stimulation of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) by dexameth. Int J Mol Sci 18 PMID: 28825630

Andersen et al (2013) A phosphoinositide 3-kinase (PI3K)-serum- and glucocorticoid-inducible kinase 1 (SGK1) pathway promotes Kv7.1 channel surface expression by inhibiting Nedd4-2 protein. J Biol Chem 288 36841 PMID: 24214981

Peng et al (2013) Spinal serum-inducible and glucocorticoid-inducible kinase 1 mediates neuropathic pain via kalirin and downstream PSD-95-dependent NR2B phosphorylation in rats. J Neurosci 33 5227 PMID: 23516288

Kaiser et al (2013) Regulation of forkhead box O1 (FOXO1) by protein kinase B and glucocorticoids: different mechanisms of induction of beta cell death in vitro. Diabetologia 56 1587 PMID: 23435785

Shin et al (2015) Phosphorylation on TRPV4 Serine 824 Regulates Interaction with STIM1. Open Biochem J 9 24 PMID: 25972993

Koeppen et al (2014) Serum- and glucocorticoid-induced protein kinase 1 (SGK1) increases the cystic fibrosis transmembrane conductance regulator (CFTR) in airway epithelial cells by phosphorylating Shank2E protein. J Clin Invest 289 17142 PMID: 24811177

Kleinewietfeld et al (2013) Sodium chloride drives autoimmune disease by the induction of pathogenic TH17 cells. Sci Rep 496 518 PMID: 23467095

Kleiner et al (2018) Activator protein-1 contributes to the NaCl-induced expression of VEGF and PlGF in RPE cells. Mol Vis 24 647 PMID: 30310263

Zhang et al (2015) Excess salt exacerbates blood-brain barrier disruption via a p38/MAPK/SGK1-dependent pathway in permanent cerebral ischemia. Cell Death Dis 5 16548 PMID: 26549644

Pastore et al (2015) SGK-1 protects kidney cells against apoptosis induced by ceramide and TNF-α. Oncotarget 6 e1890 PMID: 26379195

Beauchamp et al (2015) A high-throughput kinome screen reveals serum/glucocorticoid-regulated kinase 1 as a therapeutic target for NF2-deficient meningiomas. J Biol Chem 6 16981 PMID: 26219339

Hernandez et al (2015) Sodium chloride inhibits the suppressive function of FOXP3+ regulatory T cells. J Neurosci 125 4212 PMID: 26524592

Mattes et al (2014) Rapid elevation of sodium transport through Ins is mediated by AKT in alveolar cells. Physiol Rep 2 e00269 PMID: 24760523

Burgon et al (2014) Serum and glucocorticoid-regulated kinase 1 regulates neutrophil clearance during inflammation resolution. J Immunol 192 1796 PMID: 24431232

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Reviews for GSK 650394

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We got expected effect.
By Ashish Juvekar on 05/05/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: HCC1937

SGK (GSK650394 10 μM)

PMID: 27402769
review image

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