Chemical Name: 2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one
Biological ActivityPD 98059 is an inhibitor of mitogen-activated protein kinase kinase (MKK / MEK). Acts by binding to the inactivated form of MEK, thereby preventing its phosphorylation by cRAF or MEK kinase (IC50 = 2-7 μM). Inhibits cell growth and proliferation in acute myelogenous leukemia (AML) cell lines; causes G1 arrest by blocking p53-dependent p21 induction. Enhances embryonic stem cell self-renewal.
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Mitogen-activated protein kinase kinase inhibition enhances nuclear proapoptotic function of p53 in acute myelogenous leukemia cells.
Kojima K, Konopleva M, Samudio IJ
Cancer Res., 2007;67(7):3210-9.
BMP4 supports self-renewal of embryonic stem cells by inhibiting mitogen-activated protein kinase pathways.
Qi et al.
PD 98059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo.
Alessi et al.
A synthetic inhibitor of the mitogen-activated protein kinase cascade.
Dudley et al.
Effects of mitogen-activated protein kinase kinase inhibitor PD 98059 on antigen challenge of guinea-pig airways in vitro.
Tsang et al.
Citations for PD 98059
The citations listed below are publications that use Tocris products. Selected citations for PD 98059 include:
96 Citations: Showing 1 - 10
Pancreatic Ins content regulation by the estrogen receptor ER alpha.
Authors: Alonso-Magdalena Et al.
PLoS One ;3:e2069
Tweety-homolog (Ttyh) Family Encodes the Pore-forming Subunits of the Swelling-dependent Volume-regulated Anion Channel (VRACswell) in the Brain.
Authors: Han Et al.
Exp Neurobiol 2019;28:183
Mel1c Mediated Monochromatic Light-Stimulated IGF-I Synthesis through the Intracellular Gαq/PKC/ERK Signaling Pathway.
Authors: Ning Et al.
Int J Mol Sci 2019;20
LRRK2 kinase plays a critical role in manganese-induced inflammation and apoptosis in microglia.
Authors: Kim Et al.
PLoS One 2019;14:e0210248
The sensitivity to Hsp90 inhibitors of both normal and oncogenically transformed cells is determined by the equilibrium between cellular quiescence and activity.
Authors: Echeverría Et al.
PLoS One 2019;14:e0208287
Secreted Amyloid Precursor Protein-Alpha Promotes Arc Protein Synthesis in Hippocampal Neurons.
Authors: Livingstone Et al.
Front Mol Neurosci 2019;12:198
Volume expansion and TRPV4 activation regulate stem cell fate in three-dimensional microenvironments.
Authors: Lee Et al.
Nat Commun 2019;10:529
Human vascular cell responses to the circulating bone hormone osteocalcin.
Authors: Millar Et al.
J Cell Physiol 2019;
The homozygous CX3CR1-M280 mutation impairs human monocyte survival.
Authors: Collar Et al.
JCI Insight 2018;3
Activation of Serotonin 5-HT7 Receptors Modulates Hippocampal Synaptic Plasticity by Stimulation of Adenylate Cyclases and Rescues Learning and Behavior in a Mouse Model of Fragile X Syndrome.
Authors: Costa Et al.
Front Mol Neurosci 2018;11:353
Chemerin-induced arterial contraction is Gi- and calcium-dependent.
Authors: Ferland Et al.
Vascul Pharmacol 2017;88:30
Follicular Stimulating Hormone Accelerates Atherogenesis by Increasing Endothelial VCAM-1 Expression.
Authors: Li Et al.
cAMP-dependent cell differentiation triggered by activated CRHR1 in hippocampal neuronal cells.
Authors: Inda Et al.
Sci Rep 2017;7:1944
Molecular mechanisms involved in the non-monotonic effect of bisphenol-a on Ca2+ entry in mouse pancreatic β-cells.
Authors: Villar-Pazos Et al.
Sci Rep 2017;7:11770
G protein-coupled receptor GPR19 regulates E-cadherin expression and invasion of breast cancer cells
Authors: Rao and Herr
Biochim Biophys Acta 2017;1864(7):1318
Cannabinoid receptor 1 contributes to sprouted innervation in endometrial ectopic growth through mitogen-activated protein kinase activation.
Brain Res 2017;1663:132
Six-transmembrane epithelial antigens of the prostate comprise a novel inflammatory nexus in patients with pustular skin disorders.
Authors: Liang Et al.
J Allergy Clin Immunol 2017;139:1217
The GABAB positive allosteric modulators CGP7930 and GS39783 stimulate ERK1/2 signalling in cellslacking functional GABAB receptors
Authors: Olianas Et al.
European Journal of Pharmacology 2016;794:135
Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells
Authors: Mou Et al.
Cell: Stem Cell 2016;19:217
Pyrrolidine dithiocarbamate activates the Nrf2 pathway in astrocytes.
Authors: Liddell Et al.
J Neuroinflammation 2016;13:49
Andrographolide induces Nrf2 and heme oxygenase 1 in astrocytes by activating p38 MAPK and ERK.
Authors: Wong Et al.
J Neuroinflammation 2016;13:251
18α-glycyrrhetinic acid lethality for neuroblastoma cells via de-regulating the Beclin-1/Bcl-2 complex and inducing apoptosis.
Authors: Rahman Et al.
Biochemical Pharmacology 2016;117:97
Endogenous 17β-OE is required for activity-dependent long-term potentiation in the striatum: interaction with the DArgic system.
Authors: Tozzi Et al.
Front Cell Neurosci 2015;9:192
The LPA1/ZEB1/miR-21-activation pathway regulates metastasis in basal breast cancer.
Authors: Sahay Et al.
Int J Mol Med 2015;6:20604
Tissue factor/factor VIIa signalling promotes cytokine-induced beta cell death and impairs glucose-stimulated Ins secretion from human pancreatic islets.
Authors: Edén Et al.
Analysis of the anti-proliferative and the pro-apoptotic efficacy of Syk inhibition in multiple myeloma.
Authors: Koerber Et al.
MAPK signaling downstream to TLR4 contributes to PacT.-induced peripheral neuropathy.
Authors: Li Et al.
Brain Behav.Immun. 2015;49:255
MFG-E8 inhibits neutrophil migration through αvβ3-integrin-dependent MAP kinase activation.
Authors: Aziz Et al.
J Neuroinflammation 2015;36:18
Different patterns of electrical activity lead to long-term potentiation by activating different intracellular pathways.
Authors: Zhu Et al.
PLoS One 2015;35:621
Dimeric dipeptide mimetics of the nerve growth factor Loop 4 and Loop 1 activate TRKA with different patterns of intracellular signal transduction.
Authors: Gudasheva Et al.
Int J Mol Sci 2015;22:106
Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.
Authors: Lin Et al.
Exp Hematol Oncol 2015;16:5555
NF-κB transcriptional activation by TNFα requires phospholipase C, extracellular signal-regulated kinase 2 and poly(ADP-ribose) polymerase-1.
Authors: Vuong Et al.
J Neurosci 2015;12:229
Synergistic effects of high dietary calcium and exogenous parathyroid hormone in promoting osteoblastic bone formation in mice.
Authors: Feng Et al.
Br J Nutr 2015;113:909
The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation.
Authors: Smith Et al.
Mol Cancer 2015;10:e0136546
Differential effects of the Toll-like receptor 2 agonists, PGN and Pam3CSK4 on anti-IgE induced human mast cell activation.
Authors: Yu Et al.
PLoS One 2014;9:e112989
Synergy between sphingosine 1-phosphate and lipopolysaccharide signaling promotes an inflammatory, angiogenic and osteogenic response in human aortic valve interstitial cells.
Authors: Fernández-Pisonero Et al.
PLoS One 2014;9:e109081
Distinct signalling pathways of murine histamine H1- and H4-receptors expressed at comparable levels in HEK293 cells.
Authors: Beermann Et al.
PLoS One 2014;9:e107481
Angiogenic growth factors augment K-Cl cotransporter expression in erythroid cells via hypoxia-inducible factor-1α.
Authors: Gonsalves Et al.
Am J Hematol 2014;89:273
Oxytocin is an age-specific circulating hormone that is necessary for muscle maintenance and regeneration.
Authors: Elabd Et al.
Nat Commun 2014;5:4082
Resolvin D2 supports MCF-7 cell proliferation via activation of estrogen receptor.
Authors: Al-Zaubai Et al.
J Pharmacol Exp Ther 2014;351:172
Central SDF-1/CXCL12 expression and its cardiovascular and sympathetic effects: the role of angiotensin II, TNF-α, and MAP kinase signaling.
Authors: Wei Et al.
Am J Physiol Heart Circ Physiol 2014;307:H1643
Synergistic regulation of glutamatergic transmission by serotonin and NE reuptake inhibitors in prefrontal cortical neurons.
Authors: Yuen Et al.
J Biol Chem 2014;289:25177
GABA(A) receptor pi (GABRP) stimulates basal-like breast cancer cell migration through activation of extracellular-regulated kinase 1/2 (ERK1/2).
Authors: Sizemore Et al.
J Biol Chem 2014;289:24102
Cross-talk between alpha1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation.
Authors: Morelli Et al.
BMC Cancer 2014;14:921
BDNF-endocannabinoid interactions at neocortical inhibitory synapses require phospholipase C signaling.
J Neurophysiol 2014;111:1008
Fibroblast growth factor-4 enhances proliferation of mouse embryonic stem cells via activation of c-Jun signaling.
Authors: Kook Et al.
PLoS One 2013;8:e71641
Activation of ErbB2 and Downstream Signalling via Rho Kinases and ERK1/2 Contributes to Diabetes-Induced Vascular Dysfunction.
Authors: Akhtar Et al.
PLoS One 2013;8:e67813
Group II metabotropic glutamate receptor agonist LY379268 regulates AMPA receptor trafficking in prefrontal cortical neurons.
Authors: Wang Et al.
Effects of Y27632 on keratinocyte procurement and wound healing.
Authors: Gandham Et al.
PLoS One 2013;38:782
Epigallocatechin gallate (EGCG) stimulates autophagy in vascular endothelial cells: a potential role for reducing lipid accumulation.
Authors: Kim Et al.
J Biol Chem 2013;288:22693
A Taiwanese Propolis Derivative Induces Apoptosis through Inducing Endoplasmic Reticular Stress and Activating Transcription Factor-3 in Human Hepatoma Cells.
Authors: Suk Et al.
Evid Based Complement Alternat Med 2013;2013:658370
Endocrine disruptors fludioxonil and fenhexamid stimulate miR-21 expression in breast cancer cells.
Authors: Teng Et al.
Toxicol Sci 2013;131:71
DA D2 receptor activation leads to an up-regulation of glial cell line-derived neurotrophic factor via Gβγ-Erk1/2-dependent induction of Zif268.
Authors: Ahmadiantehrani and Ron
J Neurochem 2013;
Ceramide 1-phosphate stimulates proliferation of C2C12 myoblasts.
Authors: Gangoiti Et al.
Inhibition of α-SMA by the ectodomain of FGFR2c attenuates lung fibrosis.
Authors: Ju Et al.
J Pharmacol Exp Ther 2012;18:992
Curcumin inhibits glutamate release from rat prefrontal nerve endings by affecting vesicle mobilization.
Authors: Lin Et al.
J Biomed Sci 2012;13:9097
Brain microvascular pericytes are immunoactive in culture: cytokine, chemokine, nitric oxide, and LRP-1 expression in response to lipopolysaccharide.
Authors: Kovac Et al.
J Biomed Sci 2011;8:139
A screen for regulators of survival of motor neuron protein levels.
Authors: Makhortova Et al.
Nat Chem Biol 2011;7:544
Saccharomyces boulardii improves intestinal cell restitution through activation of the α2β1 integrin collagen receptor.
Authors: Canonici Et al.
Exp Cell Res 2011;6:e18427
Calcium/calmodulin-dependent protein kinase II mediates group I metabotropic glutamate receptor-dependent protein synthesis and long-term depression in rat hippocampus.
Authors: Mockett Et al.
J Neurosci 2011;31:7380
Reversible differentiation of myofibroblasts by MyoD.
Authors: Hecker Et al.
Br J Pharmacol 2011;317:1914
Wnt5a-DA D2 receptor interactions regulate DA neuron development via extracellular signal-regulated kinase (ERK) activation.
Authors: Yoon Et al.
PLoS One 2011;286:15641
Stanniocalcin-1 promotes tumor angiogenesis through up-regulation of VEGF in gastric cancer cells.
Authors: He Et al.
Mol Med 2011;18:39
IL-32gamma induces the maturation of dendritic cells with Th1- and Th17-polarizing ability through enhanced IL-12 and IL-6 production.
Authors: Jung Et al.
J Immunol 2011;186:6848
Carnosic acid induces the NAD(P)H: quinone oxidoreductase 1 expression in rat clone 9 cells through the p38/nuclear factor erythroid-2 related factor 2 pathway.
Authors: Tsai Et al.
J Nutr 2011;141:2119
Neurotoxicity induced by okadaic acid in the human neuroblastoma SH-SY5Y line can be differentially prevented by α7 and β2* nicotinic stimulation.
Authors: Barrio Et al.
Toxicol Sci 2011;123:193
β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.
Authors: Meitzen Et al.
J Neurochem 2011;116:984
Hyperactivation of NF-κB via the MEK signaling is indispensable for the inhibitory effect of cAMP on DNA damage-induced cell death.
Authors: Kloster Et al.
Mol Cancer 2011;10:45
Extranuclear estrogen receptors mediate the neuroprotective effects of estrogen in the rat hippocampus.
Authors: Yang Et al.
PLoS One 2010;5:e9851
Pharmacological and genetic accumulation of hypoxia-inducible factor-1alpha enhances excitatory synaptic transmission in hippocampal neurons through the production of vascular endothelial growth factor.
Authors: Huang Et al.
J Neurosci 2010;30:6080
Bone morphogenic protein-4 impairs endothelial function through oxidative stress-dependent cyclooxygenase-2 upregulation: implications on hypertension.
Authors: Wong Et al.
Circ Res 2010;107:984
Disassembly of shank and homer synaptic clusters is driven by soluble beta-amyloid(1-40) through divergent NMDAR-dependent signalling pathways.
Authors: Roselli Et al.
PLoS One 2009;4:e6011
BC1 regulation of metabotropic glutamate receptor-mediated neuronal excitability.
Authors: Zhong Et al.
J Neurosci 2009;29:9977
Glucocorticoid effects on memory consolidation depend on functional interactions between the medial prefrontal cortex and basolateral amygdala.
Authors: Roozendaal Et al.
J Neurosci 2009;29:14299
PLZF is a regulator of homeostatic and cytokine-induced myeloid development.
Authors: Doulatov Et al.
Genes Dev 2009;23:2076
The kinase inhibitors suni. and sora. differentially affect NK cell antitumor reactivity in vitro.
Authors: Krusch Et al.
J Immunol 2009;183:8286
Ethanol augments RANTES/CCL5 expression in rat liver sinusoidal endothelial cells and human endothelial cells via activation of NF-kappa B, HIF-1 alpha, and AP-1.
Authors: Yeligar Et al.
J Immunol 2009;183:5964
Soy phytoestrogens are neuroprotective against stroke-like injury in vitro.
Authors: Schreihofer and Redmond
J Endocrinol 2009;158:602
Transcriptional regulation of monocyte chemotactic protein-1 release by endothelin-1 in human airway smooth muscle cells involves NF-kappaB and AP-1.
Authors: Sutcliffe Et al.
Br J Pharmacol 2009;157:436
Synergistic effect of ERK inhibition on tetrandrine-induced apoptosis in A549 human lung carcinoma cells.
Authors: Cho Et al.
J Vet Sci 2009;10:23
Mitogen-activated protein kinases mediate upregulation of hypothalamic angiotensin II type 1 receptors in heart failure rats.
Authors: Wei Et al.
Reactive oxygen species stabilize hypoxia-inducible factor-1 alpha protein and stimulate transcriptional activity via AMP-activated protein kinase in DU145 human prostate cancer cells.
Authors: Jung Et al.
Inhibition of AMP-activated protein kinase sensitizes cancer cells to cisplatin-induced apoptosis via hyper-induction of p53.
Authors: Kim Et al.
J Biol Chem 2008;283:3731
Differential enhancement of leukaemia cell differentiation without elevation of intracellular calcium by plant-derived sesquiterpene lactone compounds.
Authors: Kim Et al.
Br J Pharmacol 2008;155:814
Regulation of DA transporter function and cell surface expression by D3 DA receptors.
Authors: Zapata Et al.
J Biol Chem 2007;282:35842
IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4.
Authors: Chung Et al.
J Endocrinol 2007;194:77
Ins induces airway smooth muscle contraction.
Authors: Schaafsma Et al.
Int J Mol Sci 2007;150:136
GSK-3beta acts downstream of PP2A and the PI 3-kinase-Akt pathway, and upstream of caspase-2 in ceramide-induced mitochondrial apoptosis.
Authors: Lin Et al.
J Cell Sci 2007;120:2935
PacT.-induced nuclear translocation of FOXO3a in breast cancer cells is mediated by c-Jun NH2-terminal kinase and Akt.
Authors: Sunters Et al.
Cancer Res 2006;66:212
Role of glycogen synthase kinase 3 β (GSK3β) in mediating the cytotoxic effects of the histone deacetylase inhibitor trichostatin A (TSA) in MCF-7 breast cancer cells.
Authors: Alao Et al.
J Biol Chem 2006;5:40
Cannabinoid receptor agonist-induced apoptosis of human prostate cancer cells LNCaP proceeds through sustained activation of ERK1/2 leading to G1 cell cycle arrest.
Authors: Sarfaraz Et al.
J Biol Chem 2006;281:39480
Direct phosphorylation and regulation of poly(ADP-ribose) polymerase-1 by extracellular signal-regulated kinases 1/2.
Authors: Kauppinen Et al.
Proc Natl Acad Sci U S A 2006;103:7136
Ischemic preconditioning protects by activating prosurvival kinases at reperfusion.
Authors: Hausenloy Et al.
Am J Physiol Heart Circ Physiol 2005;288:H971
Ob receptor in rabbit ovary and leptin in vitro regulation of corpora lutea.
Authors: Zerani Et al.
J Neuroinflammation 2004;183:279
IL-13-induced changes in the goblet cell density of human bronchial epithelial cell cultures: MAP kinase and phosphatidylinositol 3-kinase regulation.
Authors: Atherton Et al.
Am J Physiol Lung Cell Mol Physiol 2003;285:L730
Delphinidin, an active compound of red wine, inhibits endothelial cell apoptosis via nitric oxide pathway and regulation of calcium homeostasis.
Authors: Martin Et al.
Br J Pharmacol 2003;139:1095
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Reviews for PD 98059
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We investigate the effect of LPA on microglia metabolic states. Trying to unravel possible pathways that maybe involved in this process, we used inhibitors of MAPKs pathway. Inhibition of ERK (PD 98059; 10µM) decreased the LPA induced activation of pAMPK (among other proteins).
The role of MAPK pathways (JNK, p38 and ERK) was studied in the LPA induced pro-inflammatory phenotype in microglia. In this case cells were incubated for the indicated time points with LPA (1µM) in the presence or absence of PD98059 (10µM) or PD184352 (10µM). A series of assays were performed. Inhibition of ERK pathway didn't seem to play a role in the LPA induced phenotype (here presented: pp65).
HL-1 cells were incubated with p38 MAPK inhibitor (10 µM SB203580, 25 µMPD169316) or p42/44 MAPK kinase inhibitor (25 µM PD98059) for 30 min prior to 15dPGJ2 treatment (15 µM, 1 h). Immunoreactive bands for pp38 and pp42/44 MAPK expressions were followed by Western blot. PD98059 completely inhibited 15d-PGJ2 induced p42/44 phosphorylation (shown in Image).
Used to treat mouse ovarian theca cells to inhibit MEK and detected by Western blot.