solo para uso en investigación

GSK650394 SGK inhibidor

Cat. No.S7209

El GSK650394 es un inhibidor de la cinasa 1 regulada por el suero y los glucocorticoides con un IC50 de 62 nM y 103 nM para SGK1 y SGK2, respectivamente.

GSK650394 SGK inhibidor Chemical Structure

Estructura química

Peso molecular: 382.45

Saltar a

Control de calidad

Lote: Pureza: 99.92%

99.92

Dianas relacionadas	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Otros SGK Inhibidores	EMD638683 PROTAC SGK3 degrader-1

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Descripción de la actividad
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
Haga clic para ver más datos experimentales de líneas celulares

Información química, almacenamiento y estabilidad

Peso molecular	382.45	Fórmula	C₂₅H₂₂N₂O₂	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	890842-28-1	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	N/A			Smiles	C1CCC(C1)C2=C(C=CC(=C2)C3=CNC4=C3C=C(C=N4)C5=CC=CC=C5)C(=O)O

Solubilidad

In vitro
Lote:

DMSO : 76 mg/mL (198.71 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción

Targets/IC₅₀/Ki	SGK1 (Cell-free assay) 62 nM SGK2 (Cell-free assay) 103 nM
In vitro	El GSK650394 inhibe el transporte epitelial mediado por SGK1 con un IC50 de 0,6 μM en el ensayo SCC. En las células LNCaP, este compuesto inhibe la potenciación mediada por andrógenos de la fosforilación de Nedd4-2 y el crecimiento celular mediado por andrógenos.Esta sustancia química contrarresta la disminución de la neurogénesis inducida por el cortisol, los cambios en la señalización de Hedgehog y la translocación nuclear del GR. [2] Inhibe la replicación del virus de la gripe al impedir la exportación de vRNP de la gripe al citoplasma de las células A549.
Ensayo de quinasa	Ensayo de proximidad por centelleo (SPA)
Ensayo de quinasa	SGK1 S422D (60-431 aa; concentración final de 0,275 μg/mL) o SGK2 (concentración final de 0,875 μg/mL) se activan mediante PDK1 (concentración final de 1,1 μg/mL) en un tampón compuesto por 50 mM Tris (pH 7,5), 0,1 mM de EGTA, 0,1 mM de EDTA, 10 mM _de MgCl₂, 0,1 % de β-mercaptoetanol, 1 mg/mL de BSA y ATP (concentración final de 0,15 mM) y se incuban durante 30 minutos a 30 °C. SGK2 se prepara exactamente como se describe para SGK1, excepto que corresponde a la proteína de longitud completa. Se prepara una solución que contiene péptido CROSStide biotinilado a una concentración final de 75 μM y γ³²P-ATP correspondiente a 2×10⁶ cpm en el tampón de reacción. En una placa de 96 pocillos, se añaden 5 μL de este compuesto a 25 μL de la mezcla enzimática activada. A esto se añaden 20 μL de la mezcla CROSStide y se incuba durante 1 h a temperatura ambiente. A continuación, se añaden 50 μL de una suspensión de 25 mg/mL de perlas SPA recubiertas de estreptavidina en PBS con 0,1 M de EDTA, pH 8,0. A continuación, se sella la placa y se centrifuga durante 8 minutos a 2000 rpm, y se detecta la señal midiendo durante 30 segundos/pocillo en un contador de centelleo Packard TopCount NXT. Los valores IC50 de la inhibición de las actividades SGK1 y SGK2 por este compuesto químico se calculan a partir de estos datos utilizando el software GraphPad Prism 3.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/18794135/ [2] https://pubmed.ncbi.nlm.nih.gov/23650397/ [3] https://pubmed.ncbi.nlm.nih.gov/23487453/

Aplicaciones

Métodos	Biomarcadores	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

Soporte técnico

Instrucciones de manipulación

Tel: +1-832-582-8158 Ext:3

Si tiene alguna otra consulta, por favor deje un mensaje.

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):