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