GSK 650394

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Cat.No. 3572 - GSK 650394 | C25H22N2O2 | CAS No. 890842-28-1
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)
Datasheet
Citations (15)
Reviews
Literature

Biological Activity

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

GSK 650394 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 382.45
Formula C25H22N2O2
Storage Store at RT
Purity ≥97% (HPLC)
CAS Number 890842-28-1
PubChem ID 25022668
InChI Key WVSBGSNVCDAMCF-UHFFFAOYSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

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

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

Certificate of Analysis / Product Datasheet
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References

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

15 Citations for GSK 650394

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

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 insulin 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

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

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

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


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Literature in this Area

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Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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