Home MAPK MEK inhibitor - AhR antagonist PD98059 For research use only.

PD98059

PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist.

PD98059 Chemical Structure

PD98059 Chemical Structure

CAS No. 167869-21-8

Purity & Quality Control

PD98059 Related Products

Signaling Pathway

MEK Signaling Pathways

MEK Signaling Pathway

Cell Data

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

Biological Activity

Description PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist.
Features Does not inhibit c-Raf phosphorylated MEK1.
Targets
AhR [1]
(Cell-free assay)		 MEK1 [1]
(Cell-free assay)
1 μM 2 μM
In vitro
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. PD98059 does not inhibit the MAPK homologues JNK and P38. PD98059 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. PD98059 inhibits PDGF-stimulated activation of MAPK and thymidine incorporation into 3T3 cells with IC50 of ~10 μM and ~7 μM, respectively. [1] PD98059 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. PD98059 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. [2] PD98059 completely blocks the nerve growth factor (NGF)-induced differentiation of PC12 cells without altering cell viability. [3] PD98059 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. [4]
Kinase Assay In vitro MEK-inhibitory activity
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.
Cell Research Cell lines K-Balb, KNRK, v-raf-3Y1, SRA/3Y1, EGFR/3T3, and K562
Concentrations Dissolved in DMSO, final concentrations ~100 μM
Incubation Time 3 dyas, or 7-10 days
Method

For monolayer growth, cells are plated into multi-well plates at 10,000-20,000/mL. Forty-eight hours later, various concentrations of PD98059 are added to the cell growth medium and incubation is continued for an additional 3 days. Cells are then removed from the wells by incubation with trypsin and enumerated with a Coulter Counter. For growth in soft agar, cells are seeded into 35-mm dishes at 5,000-10,000 cells per dish with growth medium containing 0.3% agar and desired concentrations of PD98059. After 7-10 days of growth, visible colonies are manually enumerated with the aid of a dissecting microscope.
Experimental Result Images 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 17482134
In Vivo
In vivo

Treatment of mice 30 minutes before focal cerebral ischemia with PD98059 protects against damage, resulting in a decrease in infarct volume. [5] Pretreated with PD98059 (10 mg/kg per i.v. injection) 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. [6] Administration of PD98059 (10 mg/kg) in mice 1 hour after carrageenan causes a reduction in all the parameters of inflammation measured. [7]
Animal Research Animal Models Male Sprague–Dawley rats with acute pancreatitis
Dosages 10 mg/kg
Administration Injection i.v.

Chemical Information & Solubility

Molecular Weight 267.28 Formula

C16H13NO3
CAS No. 167869-21-8 SDF Download PD98059 SDF
Smiles COC1=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 46 mg/mL ( (172.1 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
How to formulate this inhibitor for i.p. injection?

Answer:
You can prepare the stock by the vehicle 30% PEG400/0.5% Tween80/5% Propylene glycol, 0.5% CMC.

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