Name: GSK-3 Inhibitor IX (BIO)
Brand: Selleck Chemicals
SKU: S7198
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Lote: Pureza: 99.93%

99.93

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 SB216763 CHIR-98014 TWS119 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
HEI-OC1	Function assay			Protection against cisplatin-induced cell death in neonatal mouse HEI-OC1 cells assessed as reduction in caspase-3/7 activity, EC50 = 0.192 μM.	30091915
SH-SY5Y	Function assay			Inhibition of GSK3-mediated beta-casein phosphorylation in human SH-SY5Y cells in presence of MG132 by Western blot analysis, IC50 = 0.29 μM.	18816110
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells after 72 hrs by MTT assay, IC50 = 1.3 μM.	19783149
IMR90	Antiproliferative assay		72 hrs	Antiproliferative activity against human IMR90 cells after 72 hrs by MTT assay, IC50 = 1.9 μM.	19783149
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 5.2 μM.	19783149
HepG2	Cytotoxicity assay		24 hrs	Cytotoxicity against human HepG2 cells assessed as cell growth inhibition after 24 hrs by alamar blue assay, IC50 = 5.3 μM.	28743492
HL60	Antiproliferative assay		5 days	Antiproliferative activity against human HL60 cells after 5 days by MTT assay, IC50 = 5.4 μM.	19783149
HuH7	Antiproliferative assay		72 hrs	Antiproliferative activity against human HuH7 cells after 72 hrs by MTT assay, IC50 = 6.2 μM.	19783149
SH-SY5Y	Cytotoxicity assay		48 hrs	Cytotoxicity against human SH-SY5Y cells after 48 hrs by MTS reduction assay, IC50 = 9 μM.	18816110
SH-SY5Y	Function assay		48 hrs	Survival of human SH-SY5Y cells after 48 hrs by MTS reduction assay, IC50 = 9.5 μM.	16854069
SH-SY5Y	Function assay			Death of human SH-SY5Y cells in absence of 20 uM Q-VD-OPh by MTS reduction assay, IC50 = 10 μM.	16854069
SH-SY5Y	Function assay			Death of human SH-SY5Y cells in presence of 20 uM Q-VD-OPh by MTS reduction assay, IC50 = 13 μM.	16854069
SH-SY5Y	Function assay		24 hrs	Survival of human SH-SY5Y cells after 24 hrs by MTS reduction assay, IC50 = 18 μM.	16854069
IMR32	Cytotoxicity assay		48 hrs	Cytotoxicity against human IMR32 cells assessed as cell viability after 48 hrs by MTT assay	21802947
SK-N-SH	Cytotoxicity assay		48 hrs	Cytotoxicity against human SK-N-SH cells assessed as cell viability after 48 hrs by MTT assay	21802947
NB39	Cytotoxicity assay		48 hrs	Cytotoxicity against human NB39 cells assessed as cell viability after 48 hrs by MTT assay	21802947
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
A549	Function assay	10 uM	15 mins	Inhibition of human mPGES1 from human A549 cells assessed as PGE2 at 10 uM after 15 mins by HPLC	24697244
HEK293	Function assay	0.5 to 1 uM		Inhibition of human GSK3 activity in HEK293 cells containing the Wnt/beta-catenin activated reporter pSuperTOPFLASH (STF293 cells) at 0.5 to 1 uM by Wnt reporter gene assay	24697244
sf9	Function assay	1 uM		Inhibition of recombinant human N-terminal GST-tagged CDK4 (S4 to E303 residues)/Cyclin D1 (Q4 to I295 residues) expressed in sf9 cells at 1 uM using RB-CTF as substrate by filter binding assay	28557430
sf9	Function assay	1 uM		Inhibition of human N-terminal GST/His6-tagged GSK3beta (M1 to T420 residues) expressed in baculovirus infected sf9 cells at 1 uM using RBER-IRStide as substrate by filter binding assay	28557430
sf9	Function assay	1 uM		Inhibition of recombinant human N-terminal GST-tagged CDK2 (M1 to L298 residues)/Cyclin A2 (M1 to L432 residues) expressed in baculovirus infected sf9 cells at 1 uM using Histone H1 as substrate by filter binding assay	28557430
sf9	Function assay	1 uM		Inhibition of recombinant human N-terminal GST-tagged CDK5 (M1 to P292 residues)/p35NCK (M1 to R307 residues) expressed in baculovirus infected sf9 cells at 1 uM using RB-CTF as substrate by filter binding assay	28557430
sf9	Function assay	1 uM		Inhibition of human N-terminal GST/His6-tagged Aurora B (A2 to A344 residues) expressed in sf9 cells at 1 uM using tetra(LRRLSLG) as substrate by filter binding assay	28557430
sf9	Function assay	1 uM		Inhibition of human N-terminal GST/His6-tagged FGFR1 (G400 to R820 residues) expressed in baculovirus infected sf9 cells at 1 uM using Poly(Glu,Tyr)4:1 as substrate by filter binding assay	28557430
sf9	Function assay	1 uM		Inhibition of recombinant human N-terminal GST/His6-tagged CDK1 (M1 to M297 residues)/Cyclin B1 (M1 to V433 residues) expressed in sf9 cells at 1 uM using RB-CTF as substrate by filter binding assay	28557430
sf9	Function assay	1 uM		Inhibition of recombinant human N-terminal GST-tagged CDK2 (M1 to L298 residues)/Cyclin E1 (M1 to A395 residues) expressed in sf9 cells at 1 uM using RB-CTF as substrate by filter binding assay	28557430
sf9	Function assay	1 uM		Inhibition of human N-terminal GST/His6-tagged Aurora A (M1 to S403 residues) expressed in baculovirus infected sf9 cells at 1 uM using tetra(LRRLSLG) as substrate by filter binding assay	28557430
sf9	Function assay	1 uM		Inhibition of human N-terminal GST-tagged Aurora B (M1 to S27 residues) expressed in sf9 cells at 1 uM using CDC25C-derived peptide as substrate by filter binding assay	28557430
HT22	Function assay	10 uM	24 hrs	Inhibition of GSK3-mediated beta casein phosphorylation in mouse HT22 cells at 10 uM after 24 hrs by Western blot analysis in presence of MG132	22998443
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Información química, almacenamiento y estabilidad

Peso molecular	356.17	Fórmula	C₁₆H₁₀BrN₃O₂	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	667463-62-9	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052			Smiles	C1=CC=C2C(=C1)C(=C(N2)C3=C(NC4=C3C=CC(=C4)Br)O)N=O

Solubilidad

In vitro
Lote:

DMSO : 71 mg/mL (199.34 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 7 mg/mL

Water : 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.
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.	3.000mg/ml (8.42mM)	Taking the 1 mL working solution as an example, add 50 μL 60 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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

Características	The first pharmacological agent shown to maintain self-renewal in human and mouse embryonic stem cells.
Targets/IC₅₀/Ki	GSK-3 (Cell-free assay) 5 nM TYK2 (Cell-free assay) 30 nM CDK5/p35 (Cell-free assay) 0.08 μM CDK2/CyclinA (Cell-free assay) 0.30 μM CDK1/CyclinB (Cell-free assay) 0.32 μM JAK3 (Cell-free assay) 0.5 μM
In vitro	BIO (6-bromoindirubin-3'-oxima) es un inhibidor específico de la glucógeno sintasa quinasa-3 (GSK-3), con una IC50 de 5 nM para GSK-3α/β, mostrando una selectividad >16 veces mayor sobre CDK5. Este compuesto interactúa dentro del bolsillo de unión del ATP de estas quinasas, reduce la fosforilación de β-catenina en un sitio específico de GSK-3 en modelos celulares, imitando estrechamente la señalización Wnt en embriones de Xenopus. En células madre embrionarias humanas y de ratón, este químico mantiene el fenotipo indiferenciado y sostiene la expresión de los factores de transcripción específicos del estado pluripotente Oct-3/4, Rex-1 y Nanog. Esta activación de Wnt mediada por el compuesto es funcionalmente reversible, ya que la retirada del compuesto conduce a programas normales de multidiferenciación en células madre embrionarias humanas y de ratón. Promueve la proliferación en cardiomiocitos de mamíferos. 6BIO es también un inhibidor pan-JAK, con valores de IC50 de 0,03, 1,5, 8,0, 0,5 μM para TYK2, JAK1, JAK2 y JAK3. Este compuesto inhibe selectivamente la fosforilación de STAT3 e induce la apoptosis de células de melanoma humano.
Ensayo de quinasa	Ensayo de quinasa
Ensayo de quinasa	Las actividades de la quinasa se ensayan en el tampón A o C a 30°C, a una concentración final de ATP de 15 μM. Se restan los valores en blanco y las actividades se calculan como pmoles de fosfato incorporado durante una incubación de 10 minutos. Los controles se realizan con diluciones apropiadas de dimetilsulfóxido. En algunos casos, la fosforilación del sustrato se evalúa mediante autorradiografía después de SDS-PAGE. GSK-3α/β se purifica de cerebro porcino mediante cromatografía de afinidad en axina inmovilizada. Se ensaya, después de una dilución 1/100 en 1 mg BSA/ml 10 mM DTT, con 5 μl de 40 μM del péptido GS-1, un sustrato específico de GSK-3, (YRRAAVPPSPSLSRHSSPHQSpEDEEE), en el tampón A, en presencia de 15 μM [γ-³²P] ATP (3.000 Ci/mmol; 1 mCi/ml) en un volumen final de 30 μl. Después de 30 minutos de incubación a 30°C, se aplican alícuotas de 25 μl del sobrenadante sobre trozos de papel de fosfocelulosa Whatman P81 de 2,5 × 3 cm, y 20 segundos después, los filtros se lavan cinco veces (durante al menos 5 minutos cada vez) en una solución de 10 ml de ácido fosfórico/litro de agua. Los filtros húmedos se cuentan en presencia de 1 ml de líquido de centelleo ACS.
In vivo	BIO suprime el crecimiento del tumor de melanoma en un modelo de xenoinjerto en ratones.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/14700633/ [2] https://pubmed.ncbi.nlm.nih.gov/14702635/ [3] https://pubmed.ncbi.nlm.nih.gov/16984885/ [4] https://pubmed.ncbi.nlm.nih.gov/21610112/

Aplicaciones

Métodos	Biomarcadores	PMID
Western blot	p-AKT / AKT / p21 / p27 p-β-catenin / β-catenin FoxO3a / FoxO1 / p-FoxO3a / p-FoxO1	27510556
Immunofluorescence	pAKT / p21 / p27 TNF-α E-cadherin / Nanog Oct3/4	27510556
Growth inhibition assay	Cell proliferation	27510556

Información del ensayo clínico

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT06337422	Not yet recruiting	Healthy Volunteer	International Bio service	September 23 2024	Phase 1
NCT04276857	Not yet recruiting	Locally Advanced Pancreatic Cancer\|Irreversible Electroporation	University of Saskatchewan	September 1 2024	Not Applicable
NCT06359041	Not yet recruiting	Generalized Myasthenia Gravis (gMG)	Cabaletta Bio	August 2024	Phase 1\|Phase 2

Soporte técnico

Instrucciones de manipulación

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

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C5=C4/X	C5:	LOG(C5):
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GSK-3 Inhibitor IX (BIO) GSK-3 inhibidor

Estructura química

Peso molecular: 356.17