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GSK650394 SGK inhibiteur

N° Cat.S7209

GSK650394 est un inhibiteur de la sérum- et glucocorticoïde-régulée kinase-1 avec une IC50 de 62 nM et 103 nM pour SGK1 et SGK2, respectivement.

GSK650394 SGK inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 382.45

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Contrôle qualité

Lot : Pureté : 99.92%

99.92

Cibles apparentées	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Autre SGK Inhibiteurs	EMD638683 PROTAC SGK3 degrader-1

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Description de lactivité
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
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
human Daoy cell	Growth inhibition assay	Inhibition of human Daoy cell growth in a cell viability assay, IC50=0.51532 μM
human BFTC-905 cell	Growth inhibition assay	Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=0.78455 μM
human KM12 cell	Growth inhibition assay	Inhibition of human KM12 cell growth in a cell viability assay, IC50=0.85069 μM
human GDM-1 cell	Growth inhibition assay	Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=0.87937 μM
human RT-112 cell	Growth inhibition assay	Inhibition of human RT-112 cell growth in a cell viability assay, IC50=1.02782 μM
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
human HUTU-80 cell	Growth inhibition assay	Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=1.30172 μM
human HGC-27 cell	Growth inhibition assay	Inhibition of human HGC-27 cell growth in a cell viability assay, IC50=1.30821 μM
human LCLC-97TM1 cell	Growth inhibition assay	Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50=1.36768 μM
human LXF-289 cell	Growth inhibition assay	Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=1.40152 μM
human HLE cell	Growth inhibition assay	Inhibition of human HLE cell growth in a cell viability assay, IC50=1.42683 μM
human RKO cell	Growth inhibition assay	Inhibition of human RKO cell growth in a cell viability assay, IC50=1.57869 μM
human SNG-M cell	Growth inhibition assay	Inhibition of human SNG-M cell growth in a cell viability assay, IC50=1.79853 μM
human MCF7 cell	Growth inhibition assay	Inhibition of human MCF7 cell growth in a cell viability assay, IC50=1.8178 μM
human A431 cell	Growth inhibition assay	Inhibition of human A431 cell growth in a cell viability assay, IC50=1.85902 μM
human BC-3 cell	Growth inhibition assay	Inhibition of human BC-3 cell growth in a cell viability assay, IC50=1.87094 μM
human A427 cell	Growth inhibition assay	Inhibition of human A427 cell growth in a cell viability assay, IC50=1.87611 μM
human SW620 cell	Growth inhibition assay	Inhibition of human SW620 cell growth in a cell viability assay, IC50=1.92816 μM
human HOS cell	Growth inhibition assay	Inhibition of human HOS cell growth in a cell viability assay, IC50=1.97312 μM
human MFH-ino cell	Growth inhibition assay	Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=1.98658 μM
human TE-12 cell	Growth inhibition assay	Inhibition of human TE-12 cell growth in a cell viability assay, IC50=1.99128 μM
human KU812 cell	Growth inhibition assay	Inhibition of human KU812 cell growth in a cell viability assay, IC50=2.1871 μM
human NCI-H2342 cell	Growth inhibition assay	Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=2.19053 μM
human BC-1 cell	Growth inhibition assay	Inhibition of human BC-1 cell growth in a cell viability assay, IC50=2.51651 μM
human TE-15 cell	Growth inhibition assay	Inhibition of human TE-15 cell growth in a cell viability assay, IC50=2.59181 μM
human T84 cell	Growth inhibition assay	Inhibition of human T84 cell growth in a cell viability assay, IC50=2.60446 μM
human SW1710 cell	Growth inhibition assay	Inhibition of human SW1710 cell growth in a cell viability assay, IC50=2.70082 μM
human CAL-12T cell	Growth inhibition assay	Inhibition of human CAL-12T cell growth in a cell viability assay, IC50=2.71158 μM
human NKM-1 cell	Growth inhibition assay	Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=2.76731 μM
human OCUB-M cell	Growth inhibition assay	Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=2.78861 μM
human 786-0 cell	Growth inhibition assay	Inhibition of human 786-0 cell growth in a cell viability assay, IC50=2.94825 μM
human EW-13 cell	Growth inhibition assay	Inhibition of human EW-13 cell growth in a cell viability assay, IC50=3.01558 μM
human 5637 cell	Growth inhibition assay	Inhibition of human 5637 cell growth in a cell viability assay, IC50=3.20669 μM
human PA-1 cell	Growth inhibition assay	Inhibition of human PA-1 cell growth in a cell viability assay, IC50=3.33083 μM
human NCI-H2122 cell	Growth inhibition assay	Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50=3.333 μM
human NCI-H460 cell	Growth inhibition assay	Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50=3.4041 μM
human CHL-1 cell	Growth inhibition assay	Inhibition of human CHL-1 cell growth in a cell viability assay, IC50=3.49665 μM
human MOLT-16 cell	Growth inhibition assay	Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=3.51555 μM
human HCT-15 cell	Growth inhibition assay	Inhibition of human HCT-15 cell growth in a cell viability assay, IC50=3.62842 μM
human G-361 cell	Growth inhibition assay	Inhibition of human G-361 cell growth in a cell viability assay, IC50=3.71745 μM
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
human ES4 cell	Growth inhibition assay	Inhibition of human ES4 cell growth in a cell viability assay, IC50=4.06069 μM
human TE-8 cell	Growth inhibition assay	Inhibition of human TE-8 cell growth in a cell viability assay, IC50=4.11582 μM
human IGR-1 cell	Growth inhibition assay	Inhibition of human IGR-1 cell growth in a cell viability assay, IC50=4.233 μM
human SW954 cell	Growth inhibition assay	Inhibition of human SW954 cell growth in a cell viability assay, IC50=4.46124 μM
human A375 cell	Growth inhibition assay	Inhibition of human A375 cell growth in a cell viability assay, IC50=5.25492 μM
human CAL-27 cell	Growth inhibition assay	Inhibition of human CAL-27 cell growth in a cell viability assay, IC50=5.33221 μM
human CAL-51 cell	Growth inhibition assay	Inhibition of human CAL-51 cell growth in a cell viability assay, IC50=5.35583 μM
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
human HT-1080 cell	Growth inhibition assay	Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=5.49347 μM
human NCI-H1299 cell	Growth inhibition assay	Inhibition of human NCI-H1299 cell growth in a cell viability assay, IC50=5.98557 μM
human HT-29 cell	Growth inhibition assay	Inhibition of human HT-29 cell growth in a cell viability assay, IC50=7.26843 μM
human A388 cell	Growth inhibition assay	Inhibition of human A388 cell growth in a cell viability assay, IC50=7.59965 μM
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
human CMK cell	Growth inhibition assay	Inhibition of human CMK cell growth in a cell viability assay, IC50=8.25377 μM
human HuP-T4 cell	Growth inhibition assay	Inhibition of human HuP-T4 cell growth in a cell viability assay, IC50=8.50234 μM
human SF126 cell	Growth inhibition assay	Inhibition of human SF126 cell growth in a cell viability assay, IC50=8.80208 μM
human MKN1 cell	Growth inhibition assay	Inhibition of human MKN1 cell growth in a cell viability assay, IC50=9.18565 μM
human LoVo cell	Growth inhibition assay	Inhibition of human LoVo cell growth in a cell viability assay, IC50=9.91292 μM
human HEL cell	Growth inhibition assay	Inhibition of human HEL cell growth in a cell viability assay, IC50=10.68 μM
human SW872 cell	Growth inhibition assay	Inhibition of human SW872 cell growth in a cell viability assay, IC50=13.6896 μM
human SW982 cell	Growth inhibition assay	Inhibition of human SW982 cell growth in a cell viability assay, IC50=13.7916 μM
human HuH-7 cell	Growth inhibition assay	Inhibition of human HuH-7 cell growth in a cell viability assay, IC50=18.2783 μM
human DU-145 cell	Growth inhibition assay	Inhibition of human DU-145 cell growth in a cell viability assay, IC50=20.4955 μM
human MC116 cell	Growth inhibition assay	Inhibition of human MC116 cell growth in a cell viability assay, IC50=21.2676 μM
human H4 cell	Growth inhibition assay	Inhibition of human H4 cell growth in a cell viability assay, IC50=21.4244 μM
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
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Informations chimiques, stockage et stabilité

Poids moléculaire	382.45	Formule	C₂₅H₂₂N₂O₂	Stockage (À partir de la date de réception)	3 ans-20°Cpoudre
N° CAS	890842-28-1	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	N/A			Smiles	C1CCC(C1)C2=C(C=CC(=C2)C3=CNC4=C3C=C(C=N4)C5=CC=CC=C5)C(=O)O

Solubilité

In vitro
Lot:

DMSO : 76 mg/mL (198.71 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
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 Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	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 Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	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.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.

Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Targets/IC₅₀/Ki	SGK1 (Cell-free assay) 62 nM SGK2 (Cell-free assay) 103 nM
In vitro	GSK650394 inhibe le transport épithélial médiatisé par SGK1 avec une CI50 de 0,6 μM dans l'essai SCC. Dans les cellules LNCaP, ce composé inhibe l'amélioration de la phosphorylation de Nedd4-2 médiatisée par les androgènes et la croissance cellulaire médiatisée par les androgènes. Ce produit chimique contrecarre la diminution de la neurogenèse induite par le Cortisol, les changements dans la signalisation Hedgehog et la translocation nucléaire de GR. [2] Il inhibe la réplication du virus de la grippe en altérant l'exportation des vRNP de la grippe dans le cytoplasme des cellules A549.
Kinase Assay	Essai de proximité par scintillation (SPA)
Kinase Assay	SGK1 S422D (60–431 aa ; concentration finale de 0,275 μg/mL) ou SGK2 (concentration finale de 0,875 μg/mL) sont activés par PDK1 (concentration finale de 1,1 μg/mL) dans un tampon composé de 50 mM Tris (pH 7,5), 0,1 mM EGTA, 0,1 mM EDTA, 10 mM MgCl₂, 0,1 % β-mercaptoéthanol, 1 mg/mL BSA et ATP (concentration finale de 0,15 mM) et incubés pendant 30 min à 30°C. SGK2 est préparé exactement comme décrit pour SGK1, sauf qu'il correspondait à la protéine pleine longueur. Une solution contenant le peptide CROSStide biotinylé à une concentration finale de 75 μM et du γ³²P-ATP correspondant à 2×10⁶ cpm est préparée dans le tampon de réaction. Dans une plaque à 96 puits, 5 μL de ce composé sont ajoutés à 25 μL du mélange enzymatique activé. À cela, 20 μL du mélange CROSStide sont ajoutés et incubés pendant 1 h à température ambiante. Ensuite, 50 μL d'une suspension de billes SPA revêtues de streptavidine à 25 mg/mL dans du PBS avec 0,1 M EDTA, pH 8,0 sont ajoutés. La plaque est ensuite scellée et centrifugée pendant 8 min à 2000 tr/min, et le signal est détecté en mesurant pendant 30 sec/puits dans un compteur à scintillation Packard TopCount NXT. Les valeurs d'IC50 de l'inhibition des activités de SGK1 et SGK2 par ce produit chimique sont calculées à partir de ces données à l'aide du logiciel GraphPad Prism 3.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/18794135/ [2] https://pubmed.ncbi.nlm.nih.gov/23650397/ [3] https://pubmed.ncbi.nlm.nih.gov/23487453/

Applications

Méthodes	Biomarqueurs	PMID
Western blot	p-SGK2 / SGK2 p-SGK1 / SGK1 c-Jun / NRF2 p21 / LC3 / p62 / PARP / Cleaved PARP	26392083
Immunofluorescence	LC3	29017179
Growth inhibition assay	Cell viability	29017179

Support technique

Instructions de manipulation

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C5=C4/X	C5:	LOG(C5):
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