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Submit ReviewGSK 650394
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)
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).
Licensing Information
Sold with the permission of GlaxoSmithKline
Compound Libraries for GSK 650394
GSK 650394 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for GSK 650394
| 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.
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 | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.24 | 100 |
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 |
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Product Datasheets for GSK 650394
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.
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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
30 Citations for GSK 650394
Citations are publications that use Tocris products. Selected citations for GSK 650394 include:
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
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
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
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
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
Dmitri et al (2019) Axonal and Myelin Neuroprotection by the Peptoid BN201 in Brain Inflammation. Neurotherapeutics 16 808-827 PMID: 30815844
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
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 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
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
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
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
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
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
Jing et al (2018) Methods for High-throughput Drug Combination Screening and Synergy Scoring. Methods Mol Biol 1711 351-398 PMID: 29344898
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
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
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Reviews for GSK 650394
Average Rating: 5 (Based on 1 Review.)
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We got expected effect.
By
Ashish Juvekar on 05/05/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: HCC1937
SGK (GSK650394 10 μM)
