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GSK650394
GSK650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2, respectively.
CAS No. 890842-28-1
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製品安全説明書
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純度：
99.92%
99.92
GSK650394関連製品
SGK阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | 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 | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | GSK650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2, respectively. | ||||
|---|---|---|---|---|---|
| Targets |
|
| 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. | ||||
| 細胞実験 | 細胞株 | LNCaP cells | ||
| 濃度 | ~10 μM | |||
| 反応時間 | 7 days | |||
| 実験の流れ | 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. | |||
| 実験結果図 | Methods | Biomarkers | 結果図 | 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 | |
化学情報
| 分子量 | 382.45 | 化学式 | C25H22N2O2 |
| CAS No. | 890842-28-1 | SDF | Download GSK650394 SDFをダウンロードする |
| Smiles | C1CCC(C1)C2=C(C=CC(=C2)C3=CNC4=C3C=C(C=N4)C5=CC=CC=C5)C(=O)O | ||
| 保管 | |||
|
In vitro |
DMSO : 76 mg/mL ( (198.71 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Water : Insoluble Ethanol : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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