GSK 650394

Cat. No. 3572

GSK 650394 C25H22N2O2 [890842-28-1]

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Chemical Name: 2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-benzoic acid

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

Technical Data

Soluble to 100 mM in DMSO
>97 %
Store at RT

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.

Certificate of Analysis / Safety Data Sheet

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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 .

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.

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

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.

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

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.

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

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.

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

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.

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.

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

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.

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Keywords: GSK 650394, supplier, Serum-, glucocorticoid-regulated, kinase, SGK1, inhibitors, inhibits, androgen, receptors, GSK650394, GlaxoSmithKline, GSK, Tocris Bioscience, Other Kinase Inhibitor products

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