Home Metabolism SGK inhibitor GSK650394 For research use only.

GSK650394

GSK650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2, respectively.

GSK650394 Chemical Structure

GSK650394 Chemical Structure

CAS No. 890842-28-1

Purity & Quality Control

GSK650394 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human M-1 cells Function assay Inhibition of SGK1-mediated epithelial sodium channel activity in human M-1 cells assessed as short circuit current by whole cell electrophysiological transepithelial experiment, IC50=0.58 μM 19497745
human MV-4-11 cell Growth inhibition assay Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=0.1649 μM SANGER
human Daoy cell Growth inhibition assay Inhibition of human Daoy cell growth in a cell viability assay, IC50=0.51532 μM SANGER
human BFTC-905 cell Growth inhibition assay Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=0.78455 μM SANGER
human KM12 cell Growth inhibition assay Inhibition of human KM12 cell growth in a cell viability assay, IC50=0.85069 μM SANGER
human GDM-1 cell Growth inhibition assay Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=0.87937 μM SANGER
human RT-112 cell Growth inhibition assay Inhibition of human RT-112 cell growth in a cell viability assay, IC50=1.02782 μM SANGER
human MONO-MAC-6 cell Growth inhibition assay Inhibition of human MONO-MAC-6 cell growth in a cell viability assay, IC50=1.18097 μM SANGER
human HUTU-80 cell Growth inhibition assay Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=1.30172 μM SANGER
human HGC-27 cell Growth inhibition assay Inhibition of human HGC-27 cell growth in a cell viability assay, IC50=1.30821 μM SANGER
human LCLC-97TM1 cell Growth inhibition assay Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50=1.36768 μM SANGER
human LXF-289 cell Growth inhibition assay Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=1.40152 μM SANGER
human HLE cell Growth inhibition assay Inhibition of human HLE cell growth in a cell viability assay, IC50=1.42683 μM SANGER
human RKO cell Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay, IC50=1.57869 μM SANGER
human SNG-M cell Growth inhibition assay Inhibition of human SNG-M cell growth in a cell viability assay, IC50=1.79853 μM SANGER
human MCF7 cell Growth inhibition assay Inhibition of human MCF7 cell growth in a cell viability assay, IC50=1.8178 μM SANGER
human A431 cell Growth inhibition assay Inhibition of human A431 cell growth in a cell viability assay, IC50=1.85902 μM SANGER
human BC-3 cell Growth inhibition assay Inhibition of human BC-3 cell growth in a cell viability assay, IC50=1.87094 μM SANGER
human A427 cell Growth inhibition assay Inhibition of human A427 cell growth in a cell viability assay, IC50=1.87611 μM SANGER
human SW620 cell Growth inhibition assay Inhibition of human SW620 cell growth in a cell viability assay, IC50=1.92816 μM SANGER
human HOS cell Growth inhibition assay Inhibition of human HOS cell growth in a cell viability assay, IC50=1.97312 μM SANGER
human MFH-ino cell Growth inhibition assay Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=1.98658 μM SANGER
human TE-12 cell Growth inhibition assay Inhibition of human TE-12 cell growth in a cell viability assay, IC50=1.99128 μM SANGER
human KU812 cell Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay, IC50=2.1871 μM SANGER
human NCI-H2342 cell Growth inhibition assay Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=2.19053 μM SANGER
human BC-1 cell Growth inhibition assay Inhibition of human BC-1 cell growth in a cell viability assay, IC50=2.51651 μM SANGER
human TE-15 cell Growth inhibition assay Inhibition of human TE-15 cell growth in a cell viability assay, IC50=2.59181 μM SANGER
human T84 cell Growth inhibition assay Inhibition of human T84 cell growth in a cell viability assay, IC50=2.60446 μM SANGER
human SW1710 cell Growth inhibition assay Inhibition of human SW1710 cell growth in a cell viability assay, IC50=2.70082 μM SANGER
human CAL-12T cell Growth inhibition assay Inhibition of human CAL-12T cell growth in a cell viability assay, IC50=2.71158 μM SANGER
human NKM-1 cell Growth inhibition assay Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=2.76731 μM SANGER
human OCUB-M cell Growth inhibition assay Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=2.78861 μM SANGER
human 786-0 cell Growth inhibition assay Inhibition of human 786-0 cell growth in a cell viability assay, IC50=2.94825 μM SANGER
human EW-13 cell Growth inhibition assay Inhibition of human EW-13 cell growth in a cell viability assay, IC50=3.01558 μM SANGER
human 5637 cell Growth inhibition assay Inhibition of human 5637 cell growth in a cell viability assay, IC50=3.20669 μM SANGER
human PA-1 cell Growth inhibition assay Inhibition of human PA-1 cell growth in a cell viability assay, IC50=3.33083 μM SANGER
human NCI-H2122 cell Growth inhibition assay Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=3.333 μM SANGER
human NCI-H460 cell Growth inhibition assay Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50=3.4041 μM SANGER
human CHL-1 cell Growth inhibition assay Inhibition of human CHL-1 cell growth in a cell viability assay, IC50=3.49665 μM SANGER
human MOLT-16 cell Growth inhibition assay Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=3.51555 μM SANGER
human HCT-15 cell Growth inhibition assay Inhibition of human HCT-15 cell growth in a cell viability assay, IC50=3.62842 μM SANGER
human G-361 cell Growth inhibition assay Inhibition of human G-361 cell growth in a cell viability assay, IC50=3.71745 μM SANGER
human SK-LU-1 cell Growth inhibition assay Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50=3.97014 μM SANGER
human ES4 cell Growth inhibition assay Inhibition of human ES4 cell growth in a cell viability assay, IC50=4.06069 μM SANGER
human TE-8 cell Growth inhibition assay Inhibition of human TE-8 cell growth in a cell viability assay, IC50=4.11582 μM SANGER
human IGR-1 cell Growth inhibition assay Inhibition of human IGR-1 cell growth in a cell viability assay, IC50=4.233 μM SANGER
human SW954 cell Growth inhibition assay Inhibition of human SW954 cell growth in a cell viability assay, IC50=4.46124 μM SANGER
human A375 cell Growth inhibition assay Inhibition of human A375 cell growth in a cell viability assay, IC50=5.25492 μM SANGER
human CAL-27 cell Growth inhibition assay Inhibition of human CAL-27 cell growth in a cell viability assay, IC50=5.33221 μM SANGER
human CAL-51 cell Growth inhibition assay Inhibition of human CAL-51 cell growth in a cell viability assay, IC50=5.35583 μM SANGER
human SK-LMS-1 cell Growth inhibition assay Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50=5.38255 μM SANGER
human HT-1080 cell Growth inhibition assay Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=5.49347 μM SANGER
human NCI-H1299 cell Growth inhibition assay Inhibition of human NCI-H1299 cell growth in a cell viability assay, IC50=5.98557 μM SANGER
human HT-29 cell Growth inhibition assay Inhibition of human HT-29 cell growth in a cell viability assay, IC50=7.26843 μM SANGER
human A388 cell Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay, IC50=7.59965 μM SANGER
human SK-MEL-30 cell Growth inhibition assay Inhibition of human SK-MEL-30 cell growth in a cell viability assay, IC50=7.97215 μM SANGER
human CMK cell Growth inhibition assay Inhibition of human CMK cell growth in a cell viability assay, IC50=8.25377 μM SANGER
human HuP-T4 cell Growth inhibition assay Inhibition of human HuP-T4 cell growth in a cell viability assay, IC50=8.50234 μM SANGER
human SF126 cell Growth inhibition assay Inhibition of human SF126 cell growth in a cell viability assay, IC50=8.80208 μM SANGER
human MKN1 cell Growth inhibition assay Inhibition of human MKN1 cell growth in a cell viability assay, IC50=9.18565 μM SANGER
human LoVo cell Growth inhibition assay Inhibition of human LoVo cell growth in a cell viability assay, IC50=9.91292 μM SANGER
human HEL cell Growth inhibition assay Inhibition of human HEL cell growth in a cell viability assay, IC50=10.68 μM SANGER
human SW872 cell Growth inhibition assay Inhibition of human SW872 cell growth in a cell viability assay, IC50=13.6896 μM SANGER
human SW982 cell Growth inhibition assay Inhibition of human SW982 cell growth in a cell viability assay, IC50=13.7916 μM SANGER
human HuH-7 cell Growth inhibition assay Inhibition of human HuH-7 cell growth in a cell viability assay, IC50=18.2783 μM SANGER
human DU-145 cell Growth inhibition assay Inhibition of human DU-145 cell growth in a cell viability assay, IC50=20.4955 μM SANGER
human MC116 cell Growth inhibition assay Inhibition of human MC116 cell growth in a cell viability assay, IC50=21.2676 μM SANGER
human H4 cell Growth inhibition assay Inhibition of human H4 cell growth in a cell viability assay, IC50=21.4244 μM SANGER
human SK-MEL-3 cell Growth inhibition assay Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=30.0228 μM SANGER
Click to View More Cell Line Experimental Data

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.
Targets
SGK1 [1]
(Cell-free assay)		 SGK2 [1]
(Cell-free assay)
62 nM 103 nM
In vitro
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]
Kinase Assay 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.
Cell Research Cell lines LNCaP cells
Concentrations ~10 μM
Incubation Time 7 days
Method LNCaP cells are plated at a density of 5,000 cells per well in 96-well plates in 100 μL PRF-RPMI 1640, supplemented with 8% CS-FBS, 0.1 mM NEAA, and 1 mM NaPyr. At day three, cells are treated with hormone with or without GSK650394 by removing 50 μL of the media and replacing this with 50 μL of PRF-RPMI 1640 with 8% CS-FBS, NEAA, NaPyr containing a 2X concentration of the appropriate hormone/inhibitor treatment. At days 5 and 7, the treatment is repeated. On the tenth day, the media is removed and the relative cell number is measured using the FluoReporter Blue assay according to the manufacturer’s instructions.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p21 / LC3 / p62 / PARP / Cleaved PARP c-Jun / NRF2 p-SGK1 / SGK1 p-SGK2 / SGK2 29017179
Immunofluorescence LC3 29017179
Growth inhibition assay Cell viability 29017179

Chemical Information & Solubility

Molecular Weight 382.45 Formula

C25H22N2O2
CAS No. 890842-28-1 SDF Download GSK650394 SDF
Smiles C1CCC(C1)C2=C(C=CC(=C2)C3=CNC4=C3C=C(C=N4)C5=CC=CC=C5)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 76 mg/mL ( (198.71 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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