Chemical Name: 2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-benzoic acid
Biological ActivityGSK 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).
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Development of a small-molecule serum- and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic.
Sherk et al.
Cancer Res., 2008;68:7475
Serum and glucocorticoid-regulated kinase 1 (SGK1) activation in breast cancer: requirement for mTORC1 activity associates with ER-alpha expression.
Hall et al.
Breast Cancer Res.Treat, 2012;135:469
Citations for GSK 650394
The citations listed below are publications that use Tocris products. Selected citations for GSK 650394 include:
17 Citations: Showing 1 - 10
Osmotic induction of cyclooxygenase-2 in RPE cells: Stimulation of inflammasome activation.
Authors: Messerschmidt Et al.
Mol Vis 2019;25:329
Activator protein-1 contributes to the NaCl-induced expression of VEGF and PlGF in RPE cells.
Authors: Kleiner Et al.
Mol Vis 2018;24:647
Signaling Cascade Involved in Rapid Stimulation of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) by dexameth.
Authors: Bossmann Et al.
Int J Mol Sci 2017;18
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.
Authors: Matschke Et al.
Radiat Oncol 2016;11:75
Phosphoinositide 3-kinase inhibitors induce DNA damage through nucleoside depletion.
Authors: Juvekar Et al.
Proc Natl Acad Sci U S A 2016;113:E4338
Phosphorylation on TRPV4 Serine 824 Regulates Interaction with STIM1.
Authors: Shin Et al.
Open Biochem J 2015;9:24
SGK-1 protects kidney cells against apoptosis induced by ceramide and TNF-α.
Authors: Pastore Et al.
A high-throughput kinome screen reveals serum/glucocorticoid-regulated kinase 1 as a therapeutic target for NF2-deficient meningiomas.
Authors: Beauchamp Et al.
J Biol Chem 2015;6:16981
Excess salt exacerbates blood-brain barrier disruption via a p38/MAPK/SGK1-dependent pathway in permanent cerebral ischemia.
Authors: Zhang Et al.
Cell Death Dis 2015;5:16548
Sodium chloride inhibits the suppressive function of FOXP3+ regulatory T cells.
Authors: Hernandez Et al.
J Neurosci 2015;125:4212
Rapid elevation of sodium transport through Ins is mediated by AKT in alveolar cells.
Authors: Mattes Et al.
Physiol Rep 2014;2:e00269
Serum- and glucocorticoid-induced protein kinase 1 (SGK1) increases the cystic fibrosis transmembrane conductance regulator (CFTR) in airway epithelial cells by phosphorylating Shank2E protein.
Authors: Koeppen Et al.
J Clin Invest 2014;289:17142
Serum and glucocorticoid-regulated kinase 1 regulates neutrophil clearance during inflammation resolution.
Authors: Burgon Et al.
J Immunol 2014;192:1796
Regulation of forkhead box O1 (FOXO1) by protein kinase B and glucocorticoids: different mechanisms of induction of beta cell death in vitro.
Authors: Kaiser Et al.
Sodium chloride drives autoimmune disease by the induction of pathogenic TH17 cells.
Authors: Kleinewietfeld Et al.
Sci Rep 2013;496:518
Spinal serum-inducible and glucocorticoid-inducible kinase 1 mediates neuropathic pain via kalirin and downstream PSD-95-dependent NR2B phosphorylation in rats.
Authors: Peng Et al.
J Neurosci 2013;33:5227
A phosphoinositide 3-kinase (PI3K)-serum- and glucocorticoid-inducible kinase 1 (SGK1) pathway promotes Kv7.1 channel surface expression by inhibiting Nedd4-2 protein.
Authors: Andersen Et al.
J Biol Chem 2013;288:36841
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SGK (GSK650394 10 μM)