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).
Licensing Information
Sold with the permission of GlaxoSmithKline
Compound Libraries
GSK 650394 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.24 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 382.45. Batch specific molecular weights may vary from batch to batch due to solvent 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
References
References are publications that support the products' biological activity.
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
Keywords: GSK 650394, supplier, Serum-, glucocorticoid-regulated, kinase, SGK1, inhibitors, inhibits, androgen, receptors, GSK650394, GlaxoSmithKline, GSK, Other, Kinases, Androgen, Receptor, Other, Kinases, Tocris Bioscience
