You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!Submit Review
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).
Sold with the permission of GlaxoSmithKline
Compound Libraries for GSK 650394
Technical Data for GSK 650394
|Storage||Store at RT|
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|
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.
|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|
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
If you know of a relevant reference for GSK 650394, please let us know.
View Related Products by Product Action
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
30 Citations for GSK 650394
Citations are publications that use Tocris products. Selected citations for GSK 650394 include:
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
Simon et al (2014) A zebrafish compound screen reveals modulation of neutrophil reverse migration as an anti-inflammatory mechanism. Sci Transl Med 6 225ra29 PMID: 24574340
Raymond A et al (2014) Activation of 3-phosphoinositide-dependent kinase 1 (PDK1) and serum- and glucocorticoid-induced protein kinase 1 (SGK1) by short-chain sphingolipid C4-ceramide rescues the trafficking defect of δF508-cystic fibrosis transmembrane conductance regulat J Biol Chem 289 35953-68 PMID: 25384981
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
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
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
Shin et al (2015) Phosphorylation on TRPV4 Serine 824 Regulates Interaction with STIM1. Open Biochem J 9 24 PMID: 25972993
Joshua L et al (2022) SGK2, 14-3-3, and HUWE1 Cooperate to Control the Localization, Stability, and Function of the Oncoprotein PTOV1. Mol Cancer Res 20 231-243 PMID: 34654719
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
Sharanpreet et al (2019) EAE-induced upregulation of mitochondrial MnSOD is associated with increases of mitochondrial SGK1 and Tom20 protein in the mouse kidney cortex. J Physiol Sci 69 723-732 PMID: 31177508
Dmitri et al (2019) Axonal and Myelin Neuroprotection by the Peptoid BN201 in Brain Inflammation. Neurotherapeutics 16 808-827 PMID: 30815844
Nobutaka et al (2019) mTORC2 links growth factor signaling with epigenetic regulation of iron metabolism in glioblastoma. J Biol Chem 294 19740-19751 PMID: 31712311
Jing et al (2018) Methods for High-throughput Drug Combination Screening and Synergy Scoring. Methods Mol Biol 1711 351-398 PMID: 29344898
Patrizia et al (2020) Serum- and glucocorticoid- inducible kinase 2, SGK2, is a novel autophagy regulator and modulates platinum drugs response in cancer cells. Oncogene 39 6370-6386 PMID: 32848212
George et al (2020) Metabolic Fingerprinting Links Oncogenic PIK3CA with Enhanced Arachidonic Acid-Derived Eicosanoids. Cell 181 1596-1611.e27 PMID: 32559461
Ji et al (2020) Salt Sensing by Serum/Glucocorticoid-Regulated Kinase 1 Promotes Th17-like Inflammatory Adaptation of Foxp3+ Regulatory T Cells. Cell Rep 30 1515-1529.e4 PMID: 32023466
Noriyuki et al (2020) Dual Regulation of Histone Methylation by mTOR Complexes Controls Glioblastoma Tumor Cell Growth via EZH2 and SAM. Mol Cancer Res 18 1142-1152 PMID: 32366675
Hiroto et al (2020) Bidirectional Regulation between NDRG1 and GSK3β Controls Tumor Growth and Is Targeted by Differentiation Inducing Factor-1 in Glioblastoma. Cancer Res 80 234-248 PMID: 31723002
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
Clinton et al (2016) The serum and glucocorticoid-regulated protein kinases (SGK) stimulate bovine herpesvirus 1 and herpes simplex virus 1 productive infection. Virus Res 222 106-112 PMID: 27297663
Do you know of a great paper that uses GSK 650394 from Tocris? Please let us know.
Reviews for GSK 650394
Average Rating: 5 (Based on 1 Review.)
Have you used GSK 650394?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
SGK (GSK650394 10 μM)
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.