Choose Your Country or Region

GSK650394

Catalog No.S7209 Purity:99.92%

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

CAS No. 890842-28-1

Purity & Quality Control

Batch: Purity: 99.92%

99.92

GSK650394 Related Products

Related Targets	SGK1 SGK2 SGK3	Click to Expand
Related Products	PROTAC SGK3 degrader-1	Click to Expand
Related Compound Libraries	Metabolism Compound Library Anti-cancer Metabolism Compound Library Glutamine Metabolism Compound Library Carbohydrate Metabolism Compound Library Lipid Metabolism Compound Library	Click to Expand

Cell Data

Cell Lines	Assay Type	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)
Kinase Assay	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

References
[1] Sherk AB, et al. Cancer Res. 2008, 68(18), 7475-7483. [2] Anacker C, et al. Proc Natl Acad Sci U S A. 2013, 110(21), 8708-8713. [3] Alamares-Sapuay JG, et al. J Virol. 2013, 87(10), 6020-6066.

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (1.31mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.800mg/ml (9.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 76 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 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.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):