GSK650394
For research use only.
Catalog No.S7209
18 publications
CAS No. 890842-28-1
GSK650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2, respectively.
2 Customer Reviews
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BV-2 cells were incubated in the absence or presence of gsk650394 (1 μM) for 30 min, followed by LPS (500 ng/ml) administration for 30 min, and then fixed. NF-κB p65 protein was visualized by indirect immunofluorescence staining using an antibody for NF-κB p65. For nuclear staining, the cells were stained with DAPI. Bar = 20 μm.
Biochem Biophys Res Commun, 2016, 478(1):53-59. GSK650394 purchased from Selleck.
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GSK650394 treatment reduces steady state levels of BoHV-1 proteins. Cells were grown prior to infection. Three hours prior to infection 25 nM of GSK650394 was added to the designated cultures. CRIB cells were infected withBoHV-1 (moi=2) and then stripped FBS added. At the designated times after infection (hours), whole cell lysate (50 ug protein) was prepared and Western Blots performedusing the designated antibodies directed against a viral protein. Arrows denote the position of bICP0 (97 kD), bICP4 (178 kD), bICP22 (45 kD), VP16 (65 kD), and the bracketdenotes various gE forms. Tubulin was used as a loading control. The lane marked M are molecular weight markers: numbers to left are the approximate size of the respectivebands. These results are representative of 4 independent experiments. The relative levels of the respective BoHV-1 proteins were estimated by comparing the intensity ofthe bands to tubulin using a BioRad ChemiDoc MP and PMI System. The value of the respective viral protein that was first detected after infection was set at 10 and the othervalues normalized to this value. ND refers to those lanes in which the viral protein was not detected. These results are representative of three independent experiments.
Virus Res, 2016, 222:106-112.. GSK650394 purchased from Selleck.
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Biological Activity
| Description | GSK650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2, respectively. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| In vitro |
GSK650394 inhibits SGK1-mediated epithelial transport with an IC50 of 0.6 μM in the SCC assay. In LNCaP cells, GSK650394 inhibits the androgen-mediated enhancement of Nedd4-2 phosphorylation and androgen-mediated cell growth. [2] GSK650394 counteracts the Cortisol-induced decrease in neurogenesis, changes in Hedgehog signaling, and GR nuclear translocation. [2] GSK 650394 inhibits replication of influenza virus by impairing the export of influenza vRNPs into the cytoplasm of A549 cells. [3] |
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| Cell Data |
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| Assay |
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Protocol
| Kinase Assay:[1] |
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Scintillation proximity assay (SPA): SGK1 S422D (60–431 aa; 0.275 μg/mL final concentration) or SGK2 (0.875 μg/mL final concentration) are 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 min at 30°C. SGK2 is 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 is prepared in the reaction buffer. In a 96-well plate, 5 μL of GSK650394 is added to 25 μL of the activated enzyme mixture. To this, 20 μL of the CROSStide mixture is added and incubated for 1 h 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 is added. The plate is then sealed and centrifuged for 8 min at 2000 rpm, and the signal is 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 GSK650394 are calculated from these data using GraphPad Prism 3 Software. |
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| Cell Research:[1] |
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Solubility (25°C)
| In vitro | DMSO | 76 mg/mL (198.71 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 382.45 |
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| Formula | C25H22N2O2 |
| CAS No. | 890842-28-1 |
| Storage |
powder in solvent |
| Synonyms | N/A |
| Smiles | C1CCC(C1)C2=C(C=CC(=C2)C3=CNC4=C3C=C(C=N4)C5=CC=CC=C5)C(=O)O |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
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| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
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Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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