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SB216763 GSK-3 inhibidor

Name: SB216763
Brand: Selleck Chemicals
SKU: S1075
Rating: 5 (93 reviews)

Cat. No.S1075

SB216763 es un potente y selectivo inhibidor de la GSK-3 con una IC50 de 34,3 nM para GSK-3α e igualmente eficaz para inhibir la GSK-3β humana. Este compuesto activa la autophagy.

SB216763 GSK-3 inhibidor Chemical Structure

Estructura química

Peso molecular: 371.22

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Control de calidad

Lote: Pureza: 99.98%

99.98

Dianas relacionadas	PI3K Akt mTOR ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Otros GSK-3 Inhibidores	CHIR-99021 (Laduviglusib) Laduviglusib (CHIR-99021) Hydrochloride CHIR-98014 TWS119 GSK-3 Inhibitor IX (BIO) LY2090314 Tideglusib SB415286 AR-A014418 IM-12

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad	PMID
HEK293	Function assay			Glycogen synthase activity of HEK293 cells, inhibition of GSK3-beta, EC50=0.2μM	12941331
HEK293	Function assay			Effective concentration of compound against glycogen synthase kinase-3 in HEK293 cells, EC50=0.2μM	15149684
MIAPaCa2	Growth inhibition assay		72 hrs	Growth inhibition of human MIAPaCa2 cells after 72 hrs by MTS assay, IC50=25μM	19338355
ST14A	Function assay		6 hrs	Inhibition of GSK-3-beta-mediated Wnt signaling in human ST14A cells assessed as increase in accumulation of beta-casein around nucleus after 6 hrs by microscopic analysis	20708937
neural precursor cells	Function assay			Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay	17417631
ReNcell VM	Antiproliferative assay	3 uM	72 hrs	Antiproliferative activity against human ReNcell VM cells assessed as reduction of cell proliferation at 3 uM after 72 hrs	20708937
HepG2	Function assay	34 uM	12 hrs	Increase in glucose incorporation in human HepG2 cells at 34 uM after 12 hrs by glucose assay	25467150
3T3L1	Function assay	34 uM	12 hrs	Increase in glucose incorporation in mouse 3T3L1 cells at 34 uM after 12 hrs by glucose assay	25467150
HepG2	Function assay	34 uM	12 hrs	Inhibition of GSK3beta in human HepG2 cells assessed as decrease in ratio of phosphorylated GS/GS at 34 uM after 12 hrs by Western blot analysis	25467150
Sf9	Function assay		30 min	Inhibition of GSK3beta (unknown origin) expressed in Sf9 cells using GS1 as substrate and [gamma32]ATP after 30 min by scinitllation counting, IC50=0.03388μM	SANGER
human HDLM-2 cell	Growth inhibition assay			Inhibition of human HDLM-2 cell growth in a cell viability assay, IC50=0.20984 μM	SANGER
human NCI-H1770 cell	Growth inhibition assay			Inhibition of human NCI-H1770 cell growth in a cell viability assay. IC50=0.29392 μM	SANGER
human HOP-62 cell	Growth inhibition assay			Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=0.85256 μM	SANGER
human JAR cell	Growth inhibition assay			Inhibition of human JAR cell growth in a cell viability assay, IC50=1.21044 μM	SANGER
human K5 cell	Growth inhibition assay			Inhibition of human K5 cell growth in a cell viability, IC50=1.53698 μM	SANGER
human MV-4-11 cell	Growth inhibition assay			Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=2.69685 μM	SANGER
human BT-549 cell	Growth inhibition assay			Inhibition of human BT-549 cell growth in a cell viability assay, IC50=5.29376 μM	SANGER
human LB2241-RCC cell	Growth inhibition assay			Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50=6.42874 μM	SANGER
human GAMG cell	Growth inhibition assay			Inhibition of human GAMG cell growth in a cell viability assay, IC50=6.65409 μM	SANGER
human HMV-II cell	Growth inhibition assay			Inhibition of human HMV-II cell growth in a cell viability assay, IC50=7.67607 μM	SANGER
human RS4-11 cell	Growth inhibition assay			Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=8.24141 μM	SANGER
human NCI-H1993 cell	Growth inhibition assay			Inhibition of human NCI-H1993 cell growth in a cell viability assay, IC50=8.36534 μM	SANGER
human IST-SL1 cell	Growth inhibition assay			Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=9.0204 μM	SANGER
human SK-OV-3 cell	Growth inhibition assay			Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=9.1002 μM	SANGER
human ESS-1 cell	Growth inhibition assay			Inhibition of human ESS-1 cell growth in a cell viability assay, IC50=9.59872 μM	SANGER
human G-361 cell	Growth inhibition assay			Inhibition of human G-361 cell growth in a cell viability assay, IC50=10.1798 μM	SANGER
human ALL-PO cell	Growth inhibition assay			Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=10.3477 μM	SANGER
human NB5 cell	Growth inhibition assay			Inhibition of human NB5 cell growth in a cell viability assay, IC50=11.2157 μM	SANGER
human DU-145 cell	Growth inhibition assay			Inhibition of human DU-145 cell growth in a cell viability assay, IC50=11.6535 μM	SANGER
human NMC-G1 cell	Growth inhibition assay			Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=11.7264 μM	SANGER
human RPMI-7951 cell	Growth inhibition assay			Inhibition of human RPMI-7951 cell growth in a cell viability assay. IC50=11.7864 μM	SANGER
human NCI-H2009 cell	Growth inhibition assay			Inhibition of human NCI-H2009 cell growth in a cell viability assay, IC50=13.2427 μM	SANGER
human LoVo cell	Growth inhibition assay			Inhibition of human LoVo cell growth in a cell viability assay, IC50=13.3771 μM	SANGER
human A2058 cell	Growth inhibition assay			Inhibition of human A2058 cell growth in a cell viability assay, IC50=13.469 μM	SANGER
human D-566MG cell	Growth inhibition assay			Inhibition of human D-566MG cell growth in a cell viability assay, IC50=13.9481 μM	SANGER
human QIMR-WIL cell	Growth inhibition assay			Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=15.6394 μM	SANGER
human S-117 cell	Growth inhibition assay			Inhibition of human S-117 cell growth in a cell viability assay, IC50=16.4022 μM	SANGER
human YH-13 cell	Growth inhibition assay			Inhibition of human YH-13 cell growth in a cell viability assay, IC50=16.6865 μM	SANGER
human IGROV-1 cell	Growth inhibition assay			Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=17.2001 μM	SANGER
human BHT-101 cell	Growth inhibition assay			Inhibition of human BHT-101 cell growth in a cell viability assay, IC50=17.6099 μM	SANGER
human MKN45 cell	Growth inhibition assay			Inhibition of human MKN45 cell growth in a cell viability assay, IC50=18.4128 μM	SANGER
human A498 cell	Growth inhibition assay			Inhibition of human A498 cell growth in a cell viability assay, IC50=19.4549 μM	SANGER
human U-266 cell	Growth inhibition assay			Inhibition of human U-266 cell growth in a cell viability assay, IC50=20.8797 μM	SANGER
human BFTC-905 cell	Growth inhibition assay			Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=21.1879 μM	SANGER
human BxPC-3 cell	Growth inhibition assay			Inhibition of human BxPC-3 cell growth in a cell viability assay, IC50=21.3554 μM	SANGER
human NCI-SNU-1 cell	Growth inhibition assay			Inhibition of human NCI-SNU-1 cell growth in a cell viability assay, IC50=21.5558 μM	SANGER
human SF539 cell	Growth inhibition assay			Inhibition of human SF539 cell growth in a cell viability assay, IC50=22.0198 μM	SANGER
human VA-ES-BJ cell	Growth inhibition assay			Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50=22.5763 μM	SANGER
human HuO-3N1 cell	Growth inhibition assay			Inhibition of human HuO-3N1 cell growth in a cell viability assay, IC50=22.6151 μM	SANGER
human EM-2 cell	Growth inhibition assay			Inhibition of human EM-2 cell growth in a cell viability assay, IC50=22.6689 μM	SANGER
human T98G cell	Growth inhibition assay			Inhibition of human T98G cell growth in a cell viability assay, IC50=23.3009 μM	SANGER
human SW1783 cell	Growth inhibition assay			Inhibition of human SW1783 cell growth in a cell viability assay, IC50=23.5243 μM	SANGER
human NKM-1 cell	Growth inhibition assay			Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=23.8512 μM	SANGER
human KOSC-2 cell	Growth inhibition assay			Inhibition of human KOSC-2 cell growth in a cell viability assay, IC50=24.1292 μM	SANGER
human SW48 cell	Growth inhibition assay			Inhibition of human SW48 cell growth in a cell viability assay, IC50=24.6067 μM	SANGER
human NCI-H28 cell	Growth inhibition assay			Inhibition of human NCI-H28 cell growth in a cell viability assay, IC50=25.2104 μM	SANGER
human 5637 cell	Growth inhibition assay			Inhibition of human 5637 cell growth in a cell viability assay, IC50=25.8111 μM	SANGER
human NB69 cell	Growth inhibition assay			Inhibition of human NB69 cell growth in a cell viability assay, IC50=26.1764 μM	SANGER
human HT-29 cell	Growth inhibition assay			Inhibition of human HT-29 cell growth in a cell viability assay, IC50=27.1752 μM	SANGER
human PFSK-1 cell	Growth inhibition assay			Inhibition of human PFSK-1 cell growth in a cell viability assay, IC50=27.593 μM	SANGER
human UACC-257 cell	Growth inhibition assay			Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=27.743 μM	SANGER
human D-423MG cell	Growth inhibition assay			Inhibition of human D-423MG cell growth in a cell viability assay, IC50=27.9106 μM	SANGER
human NH-12 cell	Growth inhibition assay			Inhibition of human NH-12 cell growth in a cell viability assay, IC50=28.4059 μM	SANGER
human DEL cell	Growth inhibition assay			Inhibition of human DEL cell growth in a cell viability assay, IC50=29.0474 μM	SANGER
human LS-513 cell	Growth inhibition assay			Inhibition of human LS-513 cell growth in a cell viability assay, IC50=30.1334 μM	SANGER
human NBsusSR cell	Growth inhibition assay			Inhibition of human NBsusSR cell growth in a cell viability assay, IC50=30.5678 μM	SANGER
human BV-173 cell	Growth inhibition assay			Inhibition of human BV-173 cell growth in a cell viability assay, IC50=30.7649 μM	SANGER
human A101D cell	Growth inhibition assay			Inhibition of human A101D cell growth in a cell viability assay, IC50=30.9784 μM	SANGER
human LU-134-A cell	Growth inhibition assay			Inhibition of human LU-134-A cell growth in a cell viability assay, IC50=31.0238 μM	SANGER
human ES3 cell	Growth inhibition assay			Inhibition of human ES3 cell growth in a cell viability assay, IC50=31.3376 μM	SANGER
human NY cell	Growth inhibition assay			Inhibition of human NY cell growth in a cell viability assay, IC50=32.2965 μM	SANGER
human NCI-H1975 cell	Growth inhibition assay			Inhibition of human NCI-H1975 cell growth in a cell viability assay, IC50=32.3582 μM	SANGER
human A704 cell	Growth inhibition assay			Inhibition of human A704 cell growth in a cell viability assay, IC50=34.2059 μM	SANGER
human SK-MEL-24 cell	Growth inhibition assay			Inhibition of human SK-MEL-24 cell growth in a cell viability assay, IC50=34.2523 μM	SANGER
human SW1088 cell	Growth inhibition assay			Inhibition of human SW1088 cell growth in a cell viability assay, IC50=34.3452 μM	SANGER
human SK-MEL-1 cell	Growth inhibition assay			Inhibition of human SK-MEL-1 cell growth in a cell viability, IC50=34.714 μM	SANGER
human MOLT-4 cell	Growth inhibition assay			Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=36.1467 μM	SANGER
human T47D cell	Growth inhibition assay			Inhibition of human T47D cell growth in a cell viability assay, IC50=37.1647 μM	SANGER
human SW1710 cell	Growth inhibition assay			Inhibition of human SW1710 cell growth in a cell viability assay, IC50=37.3608 μM	SANGER
human MKN7 cell	Growth inhibition assay			Inhibition of human MKN7 cell growth in a cell viability assay, IC50=38.0909 μM	SANGER
human CAL-72 cell	Growth inhibition assay			Inhibition of human CAL-72 cell growth in a cell viability assay, IC50=38.1178 μM	SANGER
human AGS cell	Growth inhibition assay			Inhibition of human AGS cell growth in a cell viability assay, IC50=38.2039 μM	SANGER
human BE-13 cell	Growth inhibition assay			Inhibition of human BE-13 cell growth in a cell viability assay, IC50=38.7783 μM	SANGER
human Calu-6 cell	Growth inhibition assay			Inhibition of human Calu-6 cell growth in a cell viability assay, IC50=39.6964 μM	SANGER
human CAL-27 cell	Growth inhibition assay			Inhibition of human CAL-27 cell growth in a cell viability assay, IC50=44.0054 μM	SANGER
human BB49-HNC cell	Growth inhibition assay			Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=44.0278 μM	SANGER
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Información química, almacenamiento y estabilidad

Peso molecular	371.22	Fórmula	C₁₉H₁₂N₂O₂Cl₂	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	280744-09-4	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	N/A			Smiles	CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=C(C=C(C=C4)Cl)Cl

Solubilidad

In vitro
Lote:

DMSO : 23 mg/mL (61.95 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.
Clear solution	5%DMSO 1 Corn oil Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	4.000mg/ml (10.78mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 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	GSK-3α (Cell-free assay) 34.3 nM GSK-3β (Cell-free assay) ~34.3 nM
In vitro	SB 216763 muestra una potencia similar para la GSK-3β con un 96% de inhibición a 10 μM, mientras que exhibe una actividad mínima contra otras 24 proteínas quinasas, incluidas PKBα y PDK1 con una IC50 de >10 μM. Este compuesto estimula la síntesis de glucógeno en células hepáticas humanas con una EC50 de 3,6 μM e induce una transcripción dosis-dependiente de un gen reportero regulado por β-catenina-LEF/TCF en células HEK293 con una inducción máxima de 2,5 veces a 5 μM. Protege las neuronas granulares cerebelosas de la muerte celular apoptótica inducida por LY-294002 o por privación de potasio de manera concentración-dependiente, con una neuroprotección máxima a 3 μM en contraste con el efecto del cloruro de litio, para el cual se requieren 10 mM. Este químico a 3 μM también previene completamente la muerte de las neuronas sensoriales del ganglio de la raíz dorsal de pollo inducida por LY-294002, independientemente del NGF. Su tratamiento a 5 μM inhibe marcadamente la fosforilación dependiente de GSK-3 de la proteína tau asociada a microtúbulos específica de neuronas en neuronas granulares cerebelosas o tau recombinante en células HEK293, e induce niveles aumentados de β-catenina citoplasmática en ambas células, imitando el efecto de la inhibición de GSK-3 mediada por Wnt. En líneas celulares de cáncer de páncreas, incluidas BXPC-3, MIA-PaCa2, PANC1, ASPC1 y CFPAC, el tratamiento con este compuesto a 25-50 μM reduce la viabilidad celular de manera dosis-dependiente y conduce a un aumento significativo de la apoptosis en un 50% a las 72 horas debido a la regulación a la baja específica de GSK-3β, mientras que no tiene efecto en las líneas celulares HMEC o WI38.
Ensayo de quinasa	ensayo de actividad de GSK-3
Ensayo de quinasa	La actividad de la quinasa GSK-3 se mide, en presencia de diversas concentraciones de SB 216763, en una mezcla de reacción que contiene concentraciones finales de 1 nM de GSK-3α humana, 50 mM de MOPS pH 7.0, 0.2 mM de EDTA, 10 mM de acetato de Mg, 7.5 mM de β-mercaptoetanol, 5% (p/v) de glicerol, 0.01% (p/v) de Tween-20, 10% (v/v) de DMSO y 28 μM de sustrato peptídico GS-2. La secuencia peptídica GS-2 corresponde a una región de la glucógeno sintasa que es fosforilada por GSK-3. El ensayo se inicia con la adición de 0.34 μCi de [³³P]γ-ATP. La concentración total de ATP es de 10 μM. Después de 30 minutos de incubación a temperatura ambiente, el ensayo se detiene con la adición de un tercio del volumen del ensayo de 2.5% (v/v) de H₃PO₄ que contiene 21 mM de ATP. Las muestras se depositan en alfombrillas de fosfocelulosa P30 y se lavan seis veces en 0.5% (v/v) de H₃PO₄. Las alfombrillas de filtro se sellan en bolsas de muestra que contienen líquido de centelleo Wallac betaplate. La incorporación de ³³P en el péptido sustrato se determina contando las alfombrillas en un contador de centelleo Wallac microbeta.
In vivo	La administración de SB 216763 a 20 mg/kg previene significativamente la inflamación pulmonar y la fibrosis subsiguiente en un modelo de inflamación y fibrosis pulmonar inducida por bleomicina (BLM) en ratones al bloquear significativamente la producción de citocinas inflamatorias MCP-1 y TNF-α por los macrófagos, y mejora significativamente la supervivencia de los ratones tratados con BLM. Este tratamiento compuesto provoca una reducción significativa de la alveolitis inducida por BLM al inhibir el daño de las células epiteliales alveolares.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/11033082/ [2] https://pubmed.ncbi.nlm.nih.gov/11279265/ [3] https://pubmed.ncbi.nlm.nih.gov/15781615/ [4] https://pubmed.ncbi.nlm.nih.gov/19959748/

Aplicaciones

Métodos	Biomarcadores	Imágenes	PMID
Western blot	c-Myb pGSK-3β / GSK-3β / E2F1 / β-catenin		21795403
Growth inhibition assay	Cell viability		24779365

Soporte técnico

Instrucciones de manipulación

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