research use only
Cat.No.S1177
| Related Targets | ERK p38 MAPK Raf JNK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase |
|---|---|
| Other MEK Inhibitors | PD0325901 (Mirdametinib) U0126-EtOH PD184352 (CI-1040) BIX 02189 Pimasertib (AS-703026) Refametinib (RDEA119) TAK-733 AZD8330 BIX 02188 SL-327 |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | 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 | ||
| Click to View More Cell Line Experimental Data | ||||||
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In vitro |
DMSO
: 46 mg/mL
(172.1 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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as vortex, ultrasound or hot water bath can be used to aid dissolving.
| Molecular Weight | 267.28 | Formula | C16H13NO3 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 167869-21-8 | Download SDF | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | COC1=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2 | ||
| Features |
Does not inhibit c-Raf phosphorylated MEK1.
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|---|---|
| Targets/IC50/Ki |
AhR
(Cell-free assay) 1 μM
MEK1
(Cell-free assay) 2 μM
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| In vitro |
PD98059 inhibits either basal MEK1 or a partially activated MEK produced by mutation of serine at residues 218 and 222 to glutamate (MEK-2E) with IC50 of 2 μM. This compound does not inhibit the MAPK homologues JNK and P38. It is highly selective against MEK, as it does not inhibit a number of other kinase activities including Raf kinase, cAMP-dependent kinase, protein kinase C, v-Src, epidermal growth factor (EGF) receptor kinase, insulin receptor kinase, PDGF receptor kinase, and phosphatidylinositol 3-kinase. This inhibitor inhibits PDGF-stimulated activation of MAPK and thymidine incorporation into 3T3 cells with IC50 of ~10 μM and ~7 μM, respectively. It potently prevents the activation of MEK1 by Raf or MEK kinase with IC50 of 4 μM, and weakly inhibits the activation of MEK2 by Raf with IC50 of 50 μM. This chemical does not inhibit the activation of MEK homologues MKK4 and RK kinase that participate in stress and interleukin-1-stimulated kinase cascades in KB and PC12 cells, and the activation of p70 S6 kinase by insulin or epidermal growth factor in Swiss 3T3 cells. It completely blocks the nerve growth factor (NGF)-induced differentiation of PC12 cells without altering cell viability. This compound inhibits the proliferation of RAW264.7 cells in the culture containing RANKL in a dose-dependent manner, resulting in an apparent decrease of TRAP-positive cells. |
| Kinase Assay |
In vitro MEK-inhibitory activity
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Incorporation of 32P into myelin basic protein (MBP) is assayed in the presence of glutathione S-transferase (GST) fusion proteins containing the 44-kDa MAPK (GST-MAPK) or the 45-kDa MEK (GST-MEK1). Assays are conducted in 50 μL of 50 mM Tris, pH 7.4/10 mM MgCl2/2 mM EGTA/10 μM [γ-32P]ATP containing 10 μg of GST-MEK1, 0.5 μg of GST-MAPK, and 40 μg of MBP. After incubation at 30°C for 15 minutes, reactions are stopped by addition of Laemmli SDS sample buffer. Phosphorylated MBP is resolved by SDS/10% PAGE.
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| In vivo |
Treatment of mice 30 minutes before focal cerebral ischemia with PD98059 protects against damage, resulting in a decrease in infarct volume. Pretreated with this compound 30 minutes before and then together with hourly cerulein injections for 3 hours significantly ameliorates cerulein-induced acute pancreatitis ipancreatitis on the basis of pancreatic wet weight and histology. Administration of this chemical (10 mg/kg) in mice 1 hour after carrageenan causes a reduction in all the parameters of inflammation measured. |
References |
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| Methods | Biomarkers | 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 |
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17482134 |
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Question 1:
How to formulate this inhibitor for i.p. injection?
Answer:
You can prepare the stock of this compound by the vehicle 30% PEG400/0.5% Tween80/5% Propylene glycol, 0.5% CMC.