Home / Other Kinase Inhibitors / GSK 650394

GSK 650394

Catalog #: 3572
30 Citations Datasheet / COA / SDS
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3572/10
3572/50
GSK 650394 | CAS No. 890842-28-1 | Other Kinase Inhibitors
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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%

Product Details
Citations (30)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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).

Technical Data

M.Wt:
382.45
Formula:
C25H22N2O2
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥97%
Storage:
Store at RT
CAS No:
890842-28-1

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.

Additional Information

Licensing Caveats:
Sold with the permission of GlaxoSmithKline

Background References

  1. Serum- and glucocorticoid-induced protein kinase 1 (SGK1) increases the cystic fibrosis transmembrane conductance regulator (CFTR) in airway epithelial cells by phosphorylating Shank2E protein.
    Koeppen K, Coutermarsh B, Madden D, Stanton B
    J Biol Chem, 2014;289(24):17142-50.
  2. Dietary Salt Exacerbates Experimental Colitis
    AL Tubbs, B Liu, TD Rogers, RB Sartor, EA Miao
    J. Immunol., 2017;0(0):.
  3. A phosphoinositide 3-kinase (PI3K)-serum- and glucocorticoid-inducible kinase 1 (SGK1) pathway promotes Kv7.1 channel surface expression by inhibiting Nedd4-2 protein.
    Andersen M, Krzystanek K, Petersen F, Bomholtz S, Olesen S, Abriel H, Jespersen T, Rasmussen H
    J Biol Chem, 2013;288(52):36841-54.
  4. Urokinase-type plasminogen activator (uPA) is critical for progression of tuberous sclerosis complex 2 (TSC2)-deficient tumors
    V Stepanova, KV Dergilev, KR Holman, YV Parfyonova, ZI Tsokolaeva, M Teter, EN Atochina-V, A Volgina, SV Zaitsev, SP Lewis, FG Zabozlaev, K Obraztsova, VP Krymskaya, DB Cines
    J. Biol. Chem., 2017;0(0):.
  5. The adherens junction protein afadin is an AKT substrate that regulates breast cancer cell migration.
    Elloul, Sivan, Kedrin, Dmitriy, Knoblauch, Nicholas, Beck, Andrew H, Toker, Alex
    Mol Cancer Res, 2014;12(3):464-76.
  6. 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
  7. 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

Product Datasheets

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Citations for GSK 650394

The citations listed below are publications that use Tocris products. Selected citations for GSK 650394 include:

30 Citations: Showing 1 - 10

  1. SGK2, 14-3-3, and HUWE1 Cooperate to Control the Localization, Stability, and Function of the Oncoprotein PTOV1.
    Authors: Joshua L Et al.
    Mol Cancer Res  2022;20:231-243
  2. Bidirectional Regulation between NDRG1 and GSK3β Controls Tumor Growth and Is Targeted by Differentiation Inducing Factor-1 in Glioblastoma.
    Authors: Hiroto Et al.
    Cancer Res  2020;80:234-248
  3. Serum- and glucocorticoid- inducible kinase 2, SGK2, is a novel autophagy regulator and modulates platinum drugs response in cancer cells.
    Authors: Patrizia Et al.
    Oncogene  2020;39:6370-6386
  4. Salt Sensing by Serum/Glucocorticoid-Regulated Kinase 1 Promotes Th17-like Inflammatory Adaptation of Foxp3+ Regulatory T Cells.
    Authors: Ji Et al.
    Cell Rep  2020;30:1515-1529.e4
  5. Dual Regulation of Histone Methylation by mTOR Complexes Controls Glioblastoma Tumor Cell Growth via EZH2 and SAM.
    Authors: Noriyuki Et al.
    Mol Cancer Res  2020;18:1142-1152
  6. Metabolic Fingerprinting Links Oncogenic PIK3CA with Enhanced Arachidonic Acid-Derived Eicosanoids.
    Authors: George Et al.
    Cell  2020;181:1596-1611.e27
  7. EAE-induced upregulation of mitochondrial MnSOD is associated with increases of mitochondrial SGK1 and Tom20 protein in the mouse kidney cortex.
    Authors: Sharanpreet Et al.
    J Physiol Sci  2019;69:723-732
  8. mTORC2 links growth factor signaling with epigenetic regulation of iron metabolism in glioblastoma.
    Authors: Nobutaka Et al.
    J Biol Chem  2019;294:19740-19751
  9. Osmotic induction of cyclooxygenase-2 in RPE cells: Stimulation of inflammasome activation.
    Authors: Messerschmidt Et al.
    Mol Vis  2019;25:329
  10. Axonal and Myelin Neuroprotection by the Peptoid BN201 in Brain Inflammation.
    Authors: Dmitri Et al.
    Neurotherapeutics  2019;16:808-827
  11. 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
  12. Methods for High-throughput Drug Combination Screening and Synergy Scoring.
    Authors: Jing Et al.
    Methods Mol Biol  2018;1711:351-398
  13. 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
  14. The serum and glucocorticoid-regulated protein kinases (SGK) stimulate bovine herpesvirus 1 and herpes simplex virus 1 productive infection.
    Authors: Clinton Et al.
    Virus Res  2016;222:106-112
  15. 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
  16. Phosphoinositide 3-kinase inhibitors induce DNA damage through nucleoside depletion.
    Authors: Juvekar Et al.
    Proc Natl Acad Sci U S A  2016;113:E4338
  17. Phosphorylation on TRPV4 Serine 824 Regulates Interaction with STIM1.
    Authors: Shin Et al.
    Open Biochem J  2015;9:24
  18. SGK-1 protects kidney cells against apoptosis induced by ceramide and TNF-α.
    Authors: Pastore Et al.
    Oncotarget  2015;6:e1890
  19. 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
  20. 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
  21. Sodium chloride inhibits the suppressive function of FOXP3+ regulatory T cells.
    Authors: Hernandez Et al.
    J Neurosci  2015;125:4212
  22. A zebrafish compound screen reveals modulation of neutrophil reverse migration as an anti-inflammatory mechanism.
    Authors: Simon Et al.
    Sci Transl Med  2014;6:225ra29
  23. Rapid elevation of sodium transport through Ins is mediated by AKT in alveolar cells.
    Authors: Mattes Et al.
    Physiol Rep  2014;2:e00269
  24. 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
    Authors: Raymond A Et al.
    J Biol Chem  2014;289:35953-68
  25. 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
  26. Serum and glucocorticoid-regulated kinase 1 regulates neutrophil clearance during inflammation resolution.
    Authors: Burgon Et al.
    J Immunol  2014;192:1796
  27. 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.
    Diabetologia  2013;56:1587
  28. Sodium chloride drives autoimmune disease by the induction of pathogenic TH17 cells.
    Authors: Kleinewietfeld Et al.
    Sci Rep  2013;496:518
  29. 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
  30. 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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