| GSK 650394SGK1 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.25%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
| Kinase experiment [1]: | |
Scintillation proximity assay (SPA) | SGK1 S422D (60-431 aa; 0.275 μg/mL final concentration) or SGK2 (0.875 μg/mL final concentration) were activated by PDK1 (1.1 μg/mL final concentration) in a buffer consisting of 50 mM Tris (pH 7.5), 0.1 mM EGTA, 0.1 mM EDTA, 10 mM MgCl2, 0.1% β-mercaptoethanol, 1 mg/mL BSA, and ATP (final concentration of 0.15 mM) and incubated for 30 mins at 30 °C. SGK2 was prepared exactly as described for SGK1, except it corresponded to the full-length protein. A solution containing biotinylated CROSStide peptide at a final concentration of 75 μM and γ32P-ATP corresponding to 2 × 106 cpm was prepared in the reaction buffer. In a 96-well plate, 5 μL of GSK 650394 was added to 25 μL of the activated enzyme mixture. To this, 20 μL of the CROSStide mixture was added and incubated for 1 hr at room temperature. Next, 50 μL of a 25 mg/mL slurry of streptavidin-coated SPA beads in PBS with 0.1 M EDTA, pH 8.0 was added. The plate was then sealed and centrifuged for 8 mins at 2000 rpm, and the signal was detected by measuring for 30 sec/well in a Packard TopCount NXT Scintillation Counter. The IC50 values of the inhibition of SGK1 and SGK2 activities by GSK 650394 were calculated from these data using GraphPad Prism 3 Software. |
| Cell experiment [1]: | |
Cell lines | LNCaP cells |
Preparation method | The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
Reacting condition | ~ 10 μM; 7 days |
Applications | In LNCaP cells, GSK 650394 inhibited androgen-mediated enhancement of Nedd4-2 phosphorylation. In addition, GSK 650394 also significantly inhibited androgen-stimulated growth of LNCaP cells, with an IC50 value of ~ 1 μM. |
References: [1]. Sherk A B, Frigo D E, Schnackenberg C G, et al. Development of a small-molecule serum-and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic. Cancer research, 2008, 68(18): 7475-7483. | |
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| Cas No. | 890842-28-1 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid | ||
| Canonical SMILES | C1CCC(C1)C2=C(C=CC(=C2)C3=CNC4=NC=C(C=C34)C5=CC=CC=C5)C(=O)O | ||
| Formula | C25H22N2O2 | M.Wt | 382.45 |
| Solubility | ≥19.1mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
GSK 650394 is a small molecule inhibitor of serum and glucocorticoid-regulated kinase 1 (SGK1) with IC50 value of 13nM [1].
Sgk1 gene is a target gene of androgen. Knockdown of SGK1 expression attenuates androgen-mediated growth of the prostate cancer cell line. Thus, the inhibition of SGK1 is a novel mechanism for the treatment of prostate cancer. GSK 650394 is a competitive inhibitor of SGK1. It shows potent inhibitory activity against the purified SGK1 with IC50 value of 13nM in a fluorescence polarization assay. In the activity-based scintillation proximity assay, GSK 650394 prevents the phosphorylation activity of SGK1 and SGK2 with IC50 values of 62nM and 103nM, respectively. Moreover, GSK 650394 suppresses the androgen-mediated increase of Nedd4-2 phosphorylation in LNCaP cells. It also significantly inhibits cell growth stimulated by androgen with IC50 value of about 1μM [1].
References:[1] Sherk A B, Frigo D E, Schnackenberg C G, et al. Development of a small-molecule serum-and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic. Cancer research, 2008, 68(18): 7475-7483.
