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Chemical Structure : GSK650394
CAS No.: 890842-28-1
Catalog No.: PC-49625Not For Human Use, Lab Use Only.
GSK650394 (GSK 650394) is a potent, competitive inhibitor of serum and glucocorticoid-regulated kinase 1 (SGK1) with IC50 of 62 nM and 103 nM for enzymatic activity of SGK1 and SGK2 repectively, in vitro activity-based scintillation proximity assay (SPA).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $188 | In stock | |
| 25 mg | $328 | In stock | |
| 100 mg | $858 | In stock | |
| 1 g | Get quote |
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GSK650394 (GSK 650394) is a potent, competitive inhibitor of serum and glucocorticoid-regulated kinase 1 (SGK1) with IC50 of 62 nM and 103 nM for enzymatic activity of SGK1 and SGK2 repectively, in vitro activity-based scintillation proximity assay (SPA).
GSK650394 inhibited SGK1-mediated epithelial transport with an IC50 of 0.6 uM in ldosterone-stimulated short circuit current cellular assay (SCC).
GSK650394 displays 60-fold selective for SGK1 over the upstream AGC kinase PDK1 and , >30-fold selectivity over Akt and other related kinases.
GSK650394 also potently inhibits CAMKK2 enzyme with pIC50 of 9.2.
GSK650394 repressed the androgen-mediated enhancement of Nedd4-2 phosphorylation in LNCaP cells, inhibited the androgen-stimulated growth of LNCaP cells with IC50 of 1 uM and completely abrogated androgen-mediated growth at 10 uM.
| M.Wt | 382.46 | |
| Formula | C25H22N2O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid |
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1. Sherk AB, et al. Cancer Res. 2008 Sep 15;68(18):7475-83.
2. Thomas SV, et al. J Biol Chem. 2011 Sep 16;286(37):32074-85.
3. Borst O, et al. Blood. 2012 Jan 5;119(1):251-61.
4. Carrow Wells, et al. Cells. 2023 Jan 11;12(2):287.
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