Catalog Number: 3572
Chemical Name: 2-Cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-benzoic acid
Biological Activity
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. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold with the permission of GlaxoSmithKline
Background References
  1. 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
  2. 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:

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

11 Citations: Showing 1 - 10
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  1. SGK-1 protects kidney cells against apoptosis induced by ceramide and TNF-α.
    Authors: Pastore Et al.
    Oncotarget 2015;6:e1890
  2. 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
  3. 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
  4. Sodium chloride inhibits the suppressive function of FOXP3+ regulatory T cells.
    Authors: Hernandez Et al.
    J Neurosci 2015;125:4212
  5. Rapid elevation of sodium transport through insulin is mediated by AKT in alveolar cells.
    Authors: Mattes Et al.
    Physiol Rep 2014;2:e00269
  6. 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
  7. Serum and glucocorticoid-regulated kinase 1 regulates neutrophil clearance during inflammation resolution.
    Authors: Burgon Et al.
    J Immunol 2014;192:1796
  8. 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
  9. Sodium chloride drives autoimmune disease by the induction of pathogenic TH17 cells.
    Authors: Kleinewietfeld Et al.
    Sci Rep 2013;496:518
  10. 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
  11. 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
Expand to show all 11 Citations

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