Chemical Name: 2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one
Biological ActivityInhibitor 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. Also available as part of the MAPK Cascade Inhibitor Tocriset™ and MAPK Inhibitor Tocriset™.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
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:
83 Citations: Showing 1 - 10
Pancreatic insulin content regulation by the estrogen receptor ER alpha.
Authors: Alonso-Magdalena Et al.
PLoS One ;3:e2069
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
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
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
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-estradiol is required for activity-dependent long-term potentiation in the striatum: interaction with the dopaminergic 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 insulin 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 paclitaxel-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 norepinephrine 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
Dopamine 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-dopamine D2 receptor interactions regulate dopamine 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 sunitinib and sorafenib 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 dopamine transporter function and cell surface expression by D3 dopamine 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
Insulin 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
Paclitaxel-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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Used to treat mouse ovarian theca cells to inhibit MEK and detected by Western blot.