solo para uso en investigación
Cat. No.S1177
| Dianas relacionadas | ERK p38 MAPK Raf JNK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase |
|---|---|
| Otros MEK Inhibidores | PD0325901 (Mirdametinib) U0126-EtOH PD184352 (CI-1040) BIX 02189 Pimasertib (AS-703026) Refametinib (RDEA119) TAK-733 AZD8330 SL-327 BIX 02188 |
| Líneas celulares | Tipo de ensayo | Concentración | Tiempo de incubación | Formulación | Descripción de la actividad | PMID |
|---|---|---|---|---|---|---|
| TE4 | Function Assay | 50 μM | 48 h | DMSO | upregulates the expression of HLA class I | 24244023 |
| MKN7 | Function Assay | 50 μM | 48 h | DMSO | increases expression of HLA-A02 or HLA-A24 molecules | 24244023 |
| OE19 | Function Assay | 50 μM | 48 h | DMSO | increases expression of HLA-A02 or HLA-A24 molecules | 24244023 |
| NCI-N87 | Function Assay | 50 μM | 48 h | DMSO | increases expression of HLA-A02 or HLA-A24 molecules | 24244023 |
| KATOIII | Function Assay | 50 μM | 48 h | DMSO | increases expression of HLA-A02 or HLA-A24 molecules | 24244023 |
| NUGC3 | Function Assay | 50 μM | 48 h | DMSO | increases expression of HLA-A02 or HLA-A24 molecules | 24244023 |
| NUGC2 | Function Assay | 50 μM | 48 h | DMSO | increases expression of HLA-A02 or HLA-A24 molecules | 24244023 |
| SGC-7901 | Apoptosis Assay | 20 μM | 24 h | inhibits CP-mediated apoptosis | 24241351 | |
| MG-63 | Function Assay | 20 μM | 0.5 h | blocks the CH-induced phosphorylated ELK1 protein expression | 24239640 | |
| ARPE-19 | Function Assay | 20 μM | 0.5 h | inhibits Apelin-induced phosphorylation of Erk and Akt | 24227918 | |
| CRL-2302 | Function Assay | 20 μM | 0.5 h | inhibits Apelin-induced phosphorylation of Erk and Akt | 24227918 | |
| MCF-7 | Apoptosis Assay | 20 μM | 1 h | increases caspase-9 enzyme activity | 24216289 | |
| MCF-7 | Function Assay | 20 μM | 1 h | abolishes expression of phosphorylated ERK co-treatment with conjugate | 24216289 | |
| 7402 | Apoptosis Assay | 30 μM | 5 d | decreases cell proliferation | 24211253 | |
| HT-29 | Function Assay | 20 μM | 48 h | reduces the BNIP3 expression pre-treated with 5-aza-dC | 24211581 | |
| DLD-1 | Function Assay | 20 μM | 48 h | reduces the BNIP3 expression pre-treated with 5-aza-dC | 24211581 | |
| 7721 | Apoptosis Assay | 30 μM | 5 d | decreases cell proliferation | 24211253 | |
| SGC7901 | Apoptosis Assay | 50 μM | 24/48/72 h | DMSO | induces apoptosis combined with JAK2 shRNA | 24178240 |
| SMMC7721 | Function Assay | 25/50 μM | 24 h | suppresses the expression of p-Akt or p-ERK1/2 | 24168056 | |
| MCF-7 | Growth Inhibition Assay | 10 μM | 48h | DMSO | reverses BNF-induced cell cycle arrest | 24163404 |
| Caco-2 | Function Assay | 50 μM | 48h | DMSO | enhances the mRNA levels of SCNN1A,FXYD3, LCT, LOX, HIF3A, ZG16, PDE6A and LGALS16 genes co-treated with Dex | 24161695 |
| HAECs | Function Assay | 10 μM | 1 h | attenuates TNF-α-stimulated ICAM-1 and VCAM-1 expression | 24134657 | |
| Ca9-22 | Function Assay | 3 μM | 1 h | abolishes the ability of HbR to induce IL-8 production | 24126532 | |
| Ca9-22 | Function Assay | 3 μM | 1/2 h | reduces HbR-induced ATF-2 phosphorylation | 24126532 | |
| AGS | Function Assay | 10 μM | 0.5 h | inhibits the upregulation of the IL-8 gene | 24106166 | |
| Caco-2 | Apoptosis Assay | 10 μM | 24 h | decreases cell apoptosis induced by 5-FU | 24095863 | |
| A549 | Function Assay | 50 μM | 2 h | blocks ERK phosphorylation mediated by 1,2-NQ | 24067727 | |
| HPMC | Function Assay | 10 μM | 48 h | reverses the changes in cell morphology induced by HGPDS | 24042838 | |
| HCT-8 | Apoptosis Assay | 10 μM | 24 h | decreases cell apoptosis induced by 5-FU | 24095863 | |
| HPMC | Apoptosis Assay | 10 μM | 24 h | reverses decrease in cell viability induced by HGPDS | 24042838 | |
| MGC803 | Apoptosis Assay | 20 μM | 1 h | inhibits apoptosis induced by IFN-α and 5′-DFUR | 24027750 | |
| SGC7901 | Apoptosis Assay | 20 μM | 1 h | inhibits apoptosis induced by IFN-α and 5′-DFUR | 24027750 | |
| G292 | Apoptosis Assay | 30 μM | 2 h | restores capsaicin-induced cell death | 24012930 | |
| COLO205 | Apoptosis Assay | 10/20/40 μM | 24 h | induces DNA ladder formation | 24019108 | |
| BxPC-3 | Function Assay | 10 μM | 6 h | increase miR-143 expression | 23973710 | |
| HPAF-II | Function Assay | 10 μM | 6 h | increase miR-143 expression | 23973710 | |
| HepG2 | Function Assay | 40 μM | 6/12 h | inhibits the increase of p-ERK1 and p-c-Jun protein expression by PL | 23942851 | |
| HL-60 | Apoptosis Assay | 50 μM | 1 h | rescues BA145 mediated apoptosis | 23948751 | |
| LNCaP | Function Assay | 10 μM | 1 h | decreases the EGF upregulated p-YB-1 | 23838318 | |
| HUVECs | Function Assay | 25 μM | 1 h | increase NF-κB p65 nuclear translocation | 23901008 | |
| HL60 | Function Assay | 20 μM | 72 h | DMSO | inhibits -induced CD11b expression | 23825585 |
| NB4 | Function Assay | 10 μM | 72 h | DMSO | inhibits -induced CD11b expression | 23825585 |
| EPOR/CR3 | Function Assay | 50 μM | 3 h | reduces EPO and/or IL-3-induced the tyrosine phosphorylation | 23820731 | |
| HUASMCs | Function Assay | 10 μM | 24 h | inhibits Ang II-induced ERK1/2 phosphorylation level | 23816468 | |
| HUASMCs | Function Assay | 10 μM | 24 h | diminishes Ang II-caused SOCS3 mRNA and protein expression | 23816468 | |
| SGC7901 | Function Assay | 10 μM | 24 h | inhibits the expression of phosphorylated ERK1/2 | 23792588 | |
| MKN45 | Growth Inhibition Assay | 10 μM | 24/48/72 h | inhibits cell growth co-treated with DAPT | 23792588 | |
| SGC7901 | Growth Inhibition Assay | 10 μM | 24/48/72 h | inhibits cell growth co-treated with DAPT | 23792588 | |
| MKN45 | Function Assay | 10 μM | 24 h | inhibits the expression of phosphorylated ERK1/2 | 23792588 | |
| SGC7901 | Apoptosis Assay | 10 μM | 24 h | increases the DAPT-induced cell apoptosis | 23792588 | |
| MKN45 | Apoptosis Assay | 10 μM | 24 h | increases the DAPT-induced cell apoptosis | 23792588 | |
| BxPC-3 cells | Growth Inhibition Assay | 20 μM | 0.5 h | inhibits VEGF-A-regulated HUVEC growth and tube formation induced by PAR-2 AP | 23764046 | |
| NB4 | Apoptosis Assay | 10/20/60 μM | 1.5 h | DMSO | decreases cell viability co-treated | 23735541 |
| HepG2 | Function Assay | 20 μM | 24 h | inhibits the HO-1 protein expression co-treated | 23707609 | |
| HUVECs | Apoptosis Assay | 2/4 μM | 24/48 h | induces cell death | 23707520 | |
| KG-1 | Apoptosis Assay | 20 μM | 12 h | enhances cell apoptosis induced by S1 | 23706691 | |
| AML 1# | Apoptosis Assay | 20 μM | 12 h | enhances cell apoptosis induced by S1 | 23706691 | |
| A2780 | Function Assay | 20 μM | 1 h | blocks DTCD-induced DR5 expression | 23696862 | |
| KYSE30 | Function Assay | 50 μM | 48 h | DMSO | upregulates the expression of HLA class I | 24244023 |
| TE5 | Function Assay | 50 μM | 48 h | DMSO | upregulates the expression of HLA class I | 24244023 |
| TE1 | Function Assay | 50 μM | 48 h | DMSO | upregulates the expression of HLA class I | 24244023 |
| TE3 | Function Assay | 50 μM | 48 h | DMSO | upregulates the expression of HLA class I | 24244023 |
| KYSE30 | Function Assay | 20/50/100 μM | 48 h | DMSO | inhibits p-Erk and wortmannin downregulated p-Akt in a dose-dependent manner | 24244023 |
| TE1 | Function Assay | 20/50/100 μM | 48 h | DMSO | inhibits p-Erk and wortmannin downregulated p-Akt in a dose-dependent manner | 24244023 |
| TE4 | Function Assay | 20/50/100 μM | 48 h | DMSO | inhibits p-Erk and wortmannin downregulated p-Akt in a dose-dependent manner | 24244023 |
| HT29 | Function Assay | 10 μM | 2 h | inhibits of JAK2, ERK1/2 and STAT3 phosphorylation | 24265293 | |
| HepG2 | Apoptosis Assay | 20 μM | 24 h | inhibits ERK1/2 phosphorylation and enhances VB1-induced apoptosis | 24247909 | |
| HepG2 | Function Assay | 20 μM | 2 h | enhances VB1-induced FOXO3a transcriptional activity | 24247909 | |
| MC-3 | Apoptosis Assay | 10 μM | 24 h | potentiated MESC-induced apoptosis in cells | 24270523 | |
| Raji | Function Assay | 10 μM | 1 h | blocks hsBAFF induced Erk1/2 phosphorylation | 24269630 | |
| Raji | Growth Inhibition Assay | 10 μM | 1 h | inhibits the basal or hsBAFF-stimulated cell proliferation and viability | 24269630 | |
| A549 | Function Assay | 30 μM | 0.5 h | DMSO | inhibits thrombin-induced C/EBPβ Thr235 phosphorylation | 24277696 |
| HCSMCs | Growth Inhibition Assay | 10 μM | 24 h | blocks FABP4-induced HCASMC proliferation | 24312381 | |
| PANC-1 | Function Assay | 20 μM | 48 h | inhibits the expression of Δ6D in response to the PPARδ agonist | 24294133 | |
| A549 | Function Assay | 30 μM | 0.5 h | DMSO | inhibits the thrombin-induced IL-8/CXCL8-Luc activity | 24277696 |
| SW480 | Function Assay | 10 μM | 20 h | DMSO | suppresses the CRT activity | 24324366 |
| HEK 293 | Function Assay | 10 μM | 5 h | DMSO | inhibits Wnt-induced β-catenin/TCF4 activity and nuclear β-catenin accumulation | 24324366 |
| HEK 293 | Function Assay | 10 μM | 5 h | DMSO | suppresses the CRT activity | 24324366 |
| HL-60 | Function Assay | 10/20 μM | 1 h | inhibits the N. chinensisextract induced differentiation into granulocytes | 24357020 | |
| HL-60 | Function Assay | 2 µM | 16 h | DMSO | inhibits the association of pS621 Raf-1 and NFATc3, and the RA-induced phosphorylation of nuclear NFATc3 | 24330068 |
| HeLa | Function Assay | 50 μM | 0.5 h | blocks TRX-1 nuclear migration and TXNIP down-regulation | 24376827 | |
| HUVECs | Function Assay | 10 μM | 1 h | inhibits the HDL reduced COX-2 expression and PGI-2 release | 24385109 | |
| MCF-7 | Function Assay | 10 μM | 10/30 min | reduces the UTP-dependent ERK phosphorylation | 24390819 | |
| HGC-27 | Apoptosis Assay | 1 µM | 1 h | suppresses RAD001 plus MK-2206-induced cell viability loss | 24416349 | |
| PC3 | Apoptosis Assay | 50 μM | 0.5 h | inhibits MHY-449-induced apoptosis | 24424889 | |
| HPAEpiCs | Function Assay | 30 μM | 1 h | inhibits TNF-α stimulated p42/p44 MAPK phosphorylation | 24441870 | |
| BeWo | Function Assay | 10 μM | 2 h | inhibits ERK1/2 | 24433846 | |
| A498 | Apoptosis Assay | 50 μM | 24 h | potentiates the pro-apoptotic effects of NC | 24508476 | |
| NHBE | Function Assay | 2/20 μM | 2 h | attenuates IL-33 stimulated CXCL8/IL-8 secretion | 24479526 | |
| A375 | Cell Invasion Assay | 10–20 µM | 24 h | reduces melanoma cell invasion | 24466036 | |
| HBMEC | Function Assay | 10 μM | 1 h | blocks VEGF-induced EphA2 expression | 24458982 | |
| HCT-15 | Function Assay | 1 h | attenuates PGE2-induced phosphorylation of Erk | 25431425 | ||
| HCT-15 | Apoptosis Assay | 1 h | abolishes the protective effects of PGE2 against curcumin-induced apoptosis | 25431425 | ||
| 786-O | Apoptosis Assay | 50 μM | 24 h | potentiates the pro-apoptotic effects of NC | 24508476 | |
| HepG2 | Growth Inhibition Assay | 20 μM | 24 h | suppresses TGF-β1-induced cell proliferation and invasion | 25560488 | |
| SW480 | Function Assay | 20 μM | 1 h | reduces the expression of ATF3 protein | 25447816 | |
| MDA-MB-231 | Function Assay | 25 μM | 2-3 h | decreases p-ERK1/2 and S100A4 expression | 25555875 | |
| HepG2 | Function Assay | 10 μM | 5 h | blocks phosphorylated MAPKs induced by exogenous TGF-β1 | 25560488 | |
| MCF-7 | Function Assay | 10 μM | 1 h | inhibits IL-18-enhanced cell migration | 25727011 | |
| H1355 | Function Assay | 25 μM | 1 h | blunts the B[a]P-induced increase in phospho-Chk1 and phospho-ERK expression | 25769181 | |
| PC12 | Function assay | Inhibition of nerve growth factor-mediated MAP kinase activity in human PC12 cells, IC50 = 2 μM. | 18077363 | |||
| HT-29 | Antiproliferative assay | 5 days | Antiproliferative activity against human HT-29 cells after 5 days by WST1 assay, IC50 = 4 μM. | 25078316 | ||
| IEC6 | Function assay | 5 mins | Inhibition of MEK1/2 in rat IEC6 cells assessed as reduction in ERK1/2 loop phosphorylation dosed 30 mins before to stimulation with 10% serum for 5 mins by immunoblotting method, IC50 = 4.2 μM. | 25078316 | ||
| NG 108-15 | Function assay | Concentration required to abolish MAPK activity in mouse neuroblastoma and rat glioma hybrid NG 108-15 cells, Activity = 10 μM. | 15537354 | |||
| PC12 | Function assay | 10 uM | 5 hrs | Activation of Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction at 10 uM after 5 hrs pretreated with JNK inhibitor SP600125 for 1 hr before compound addition by Western blot analysis | 21345685 | |
| PC12 | Function assay | 10 uM | 5 hrs | Activation of Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction at 10 uM after 5 hrs pretreated with MEK2 inhibitor U0126 for 1 hr before compound addition by Western blot analysis | 21345685 | |
| PC12 | Function assay | 10 uM | 5 hrs | Activation of Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction at 10 uM after 5 hrs pretreated with MEK1 inhibitor PD98059 for 1 hr before compound addition by Western blot analysis | 21345685 | |
| HeLa | Function assay | 20 uM | 3 hrs | Inhibition of ERK1/2 phosphorylation in human HeLa cells at 20 uM after 3 hrs by Western blotting analysis | 23570615 | |
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD 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 | |||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | |||
| MDA-MB-231 | Function assay | 50 uM | Downregulation of MMP2 in human MDA-MB-231 cells at 50 uM by Western blot analysis | 22926226 | ||
| MDA-MB-231 | Function assay | 50 uM | Downregulation of MMP9 in human MDA-MB-231 cells at 50 uM by Western blot analysis | 22926226 | ||
| Haga clic para ver más datos experimentales de líneas celulares | ||||||
| Peso molecular | 267.28 | Fórmula | C16H13NO3 |
Almacenamiento (Desde la fecha de recepción) | |
|---|---|---|---|---|---|
| Nº CAS | 167869-21-8 | Descargar SDF | Almacenamiento de soluciones madre |
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| Sinónimos | N/A | Smiles | COC1=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2 | ||
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In vitro |
DMSO
: 46 mg/mL
(172.1 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
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Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)
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.)
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.
| Características |
Does not inhibit c-Raf phosphorylated MEK1.
|
|---|---|
| Targets/IC50/Ki |
AhR
(Cell-free assay) 1 μM
MEK1
(Cell-free assay) 2 μM
|
| In vitro |
PD98059 inhibe tanto la MEK1 basal como una MEK parcialmente activada producida por la mutación de la serina en los residuos 218 y 222 a glutamato (MEK-2E) con una CI50 de 2 μM. Este compuesto no inhibe los homólogos de MAPK JNK y P38. Es altamente selectivo contra MEK, ya que no inhibe una serie de otras actividades quinasa, incluyendo la quinasa Raf, la quinasa dependiente de cAMP, la proteína quinasa C, v-Src, la quinasa del receptor del factor de crecimiento epidérmico (EGF), la quinasa del receptor de insulina, la quinasa del receptor de PDGF y la fosfatidilinositol 3-quinasa. Este inhibidor inhibe la activación de MAPK estimulada por PDGF y la incorporación de timidina en células 3T3 con una CI50 de ~10 μM y ~7 μM, respectivamente. Previene potentemente la activación de MEK1 por Raf o MEK quinasa con una CI50 de 4 μM, e inhibe débilmente la activación de MEK2 por Raf con una CI50 de 50 μM. Esta sustancia química no inhibe la activación de los homólogos de MEK MKK4 y RK quinasa que participan en las cascadas de quinasas estimuladas por el estrés y la interleucina-1 en células KB y PC12, ni la activación de la p70 S6 quinasa por insulina o factor de crecimiento epidérmico en células Swiss 3T3. Bloquea completamente la diferenciación de células PC12 inducida por el factor de crecimiento nervioso (NGF) sin alterar la viabilidad celular. Este compuesto inhibe la proliferación de células RAW264.7 en el cultivo que contiene RANKL de manera dosis-dependiente, lo que resulta en una disminución aparente de las células TRAP-positivas. |
| Ensayo de quinasa |
Actividad inhibidora de MEK in vitro
|
|
Se ensaya la incorporación de 32P en la proteína básica de la mielina (MBP) en presencia de proteínas de fusión de glutatión S-transferasa (GST) que contienen la MAPK de 44 kDa (GST-MAPK) o la MEK de 45 kDa (GST-MEK1). Los ensayos se realizan en 50 μL de 50 mM Tris, pH 7.4/10 mM MgCl2/2 mM EGTA/10 μM [γ-32P]ATP que contienen 10 μg de GST-MEK1, 0.5 μg de GST-MAPK y 40 μg de MBP. Después de la incubación a 30°C durante 15 minutos, las reacciones se detienen mediante la adición de tampón de muestra SDS de Laemmli. La MBP fosforilada se resuelve mediante SDS/PAGE al 10%.
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| In vivo |
El tratamiento de ratones 30 minutos antes de la isquemia cerebral focal con PD98059 protege contra el daño, lo que resulta en una disminución del volumen del infarto. El pretratamiento con este compuesto 30 minutos antes y luego junto con inyecciones horarias de ceruleína durante 3 horas mejora significativamente la pancreatitis aguda inducida por ceruleína, según el peso húmedo pancreático y la histología. La administración de este químico (10 mg/kg) en ratones 1 hora después de la carragenina provoca una reducción en todos los parámetros de inflamación medidos. |
Referencias |
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| Métodos | Biomarcadores | Imágenes | PMID |
|---|---|---|---|
| Western blot | c-Jun / α-tubulin / p-ERK / ERK / p-AKT / AKT p-JNK / JNK / Cyclin D1 p-HER2 / HER2 MMP9 / XIAP / VEGF |
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17482134 |
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Pregunta 1:
How to formulate this inhibitor for i.p. injection?
Respuesta:
You can prepare the stock of this compound by the vehicle 30% PEG400/0.5% Tween80/5% Propylene glycol, 0.5% CMC.