pour la recherche uniquement
Réf. CatalogueS1177
| Cibles apparentées | ERK p38 MAPK Raf JNK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase |
|---|---|
| Autre MEK Inhibiteurs | PD0325901 (Mirdametinib) U0126-EtOH PD184352 (CI-1040) BIX 02189 Pimasertib (AS-703026) Refametinib (RDEA119) TAK-733 AZD8330 SL-327 BIX 02188 |
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | 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 | ||
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
| Poids moléculaire | 267.28 | Formule | C16H13NO3 |
Stockage (À compter de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 167869-21-8 | Télécharger le SDF | Stockage des solutions mères |
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| Synonymes | N/A | Smiles | COC1=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2 | ||
|
In vitro |
DMSO
: 46 mg/mL
(172.1 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
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Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)
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, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.
Note : 1. Veuillez vous assurer 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 chaud peuvent être utilisées pour faciliter la dissolution.
| Caractéristiques |
Does not inhibit c-Raf phosphorylated MEK1.
|
|---|---|
| Targets/IC50/Ki |
AhR
(Cell-free assay) 1 μM
MEK1
(Cell-free assay) 2 μM
|
| In vitro |
Le PD98059 inhibe la MEK1 basale ou une MEK partiellement activée produite par mutation de la sérine aux résidus 218 et 222 en glutamate (MEK-2E) avec une CI50 de 2 μM. Ce composé n'inhibe pas les homologues de MAPK, JNK et P38. Il est très sélectif contre la MEK, car il n'inhibe pas un certain nombre d'autres activités kinases, y compris la Raf kinase, la kinase dépendante de l'AMPc, la protéine kinase C, v-Src, la kinase du récepteur du facteur de croissance épidermique (EGF), la kinase du récepteur de l'insuline, la kinase du récepteur du PDGF et la phosphatidylinositol 3-kinase. Cet inhibiteur inhibe l'activation de MAPK stimulée par le PDGF et l'incorporation de thymidine dans les cellules 3T3 avec une CI50 d'environ 10 μM et environ 7 μM, respectivement. Il prévient puissamment l'activation de MEK1 par Raf ou MEK kinase avec une CI50 de 4 μM, et inhibe faiblement l'activation de MEK2 par Raf avec une CI50 de 50 μM. Ce produit chimique n'inhibe pas l'activation des homologues de MEK MKK4 et RK kinase qui participent aux cascades de kinases stimulées par le stress et l'interleukine-1 dans les cellules KB et PC12, et l'activation de la p70 S6 kinase par l'insuline ou le facteur de croissance épidermique dans les cellules Swiss 3T3. Il bloque complètement la différenciation des cellules PC12 induite par le facteur de croissance nerveuse (NGF) sans altérer la viabilité cellulaire. Ce composé inhibe la prolifération des cellules RAW264.7 en culture contenant du RANKL de manière dose-dépendante, entraînant une diminution apparente des cellules positives au TRAP. |
| Essai kinase |
Activité inhibitrice de MEK in vitro
|
|
L'incorporation de 32P dans la protéine basique de la myéline (MBP) est mesurée en présence de protéines de fusion de la glutathion S-transférase (GST) contenant la MAPK de 44 kDa (GST-MAPK) ou la MEK de 45 kDa (GST-MEK1). Les essais sont effectués dans 50 μL de 50 mM Tris, pH 7,4/10 mM MgCl2/2 mM EGTA/10 μM [γ-32P]ATP contenant 10 μg de GST-MEK1, 0,5 μg de GST-MAPK et 40 μg de MBP. Après incubation à 30°C pendant 15 minutes, les réactions sont arrêtées par addition de tampon d'échantillon SDS de Laemmli. La MBP phosphorylée est résolue par SDS/PAGE à 10%.
|
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| In vivo |
Le traitement des souris 30 minutes avant l'ischémie cérébrale focale avec du PD98059 protège contre les dommages, entraînant une diminution du volume de l'infarctus. Un prétraitement avec ce composé 30 minutes avant, puis en même temps que des injections horaires de céruléine pendant 3 heures, améliore significativement la pancréatite aiguë induite par la céruléine sur la base du poids humide et de l'histologie du pancréas. L'administration de ce produit chimique (10 mg/kg) chez les souris 1 heure après la carragénine provoque une réduction de tous les paramètres d'inflammation mesurés. |
Références |
|
| Méthodes | Biomarqueurs | Images | PMID |
|---|---|---|---|
| Western blot | c-Jun / α-tubulin / p-ERK / ERK / p-AKT / AKT p-JNK / JNK / Cyclin D1 p-HER2 / HER2 MMP9 / XIAP / VEGF |
|
17482134 |
Tel: +1-832-582-8158 Ext:3
Si vous avez dautres questions, veuillez laisser un message.
Question 1:
How to formulate this inhibitor for i.p. injection?
Réponse :
You can prepare the stock of this compound by the vehicle 30% PEG400/0.5% Tween80/5% Propylene glycol, 0.5% CMC.