PD 98059

Catalog # Availability Size / Price Qty
1213/10
1213/50
1213/1
MEK Inhibitors Small Molecule
1 Image
Description: MEK inhibitor

Chemical Name: 2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one

Purity: ≥98%

Product Details
Citations (92)
Reviews (4)

Biological Activity

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. Also available as part of the MAPK Cascade Inhibitor Tocriset™ and MAPK Inhibitor Tocriset™.

Technical Data

M.Wt:
267.28
Formula:
C16H13NO3
Solubility:
Soluble to 25 mM in DMSO and to 5 mM in ethanol
Purity:
≥98%
Storage:
Store at RT
CAS No:
167869-21-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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Citations for PD 98059

The citations listed below are publications that use Tocris products. Selected citations for PD 98059 include:

92 Citations: Showing 1 - 10

  1. Pancreatic Ins content regulation by the estrogen receptor ER alpha.
    Authors: Alonso-Magdalena Et al.
    PLoS One  ;3:e2069
  2. LRRK2 kinase plays a critical role in manganese-induced inflammation and apoptosis in microglia.
    Authors: Kim Et al.
    PLoS One  2019;14:e0210248
  3. 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
  4. Volume expansion and TRPV4 activation regulate stem cell fate in three-dimensional microenvironments.
    Authors: Lee Et al.
    Nat Commun  2019;10:529
  5. The homozygous CX3CR1-M280 mutation impairs human monocyte survival.
    Authors: Collar Et al.
    JCI Insight  2018;3
  6. 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
  7. Chemerin-induced arterial contraction is Gi- and calcium-dependent.
    Authors: Ferland Et al.
    Vascul Pharmacol  2017;88:30
  8. Follicular Stimulating Hormone Accelerates Atherogenesis by Increasing Endothelial VCAM-1 Expression.
    Authors: Li Et al.
    Theranostics  2017;7:4671
  9. cAMP-dependent cell differentiation triggered by activated CRHR1 in hippocampal neuronal cells.
    Authors: Inda Et al.
    Sci Rep  2017;7:1944
  10. 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
  11. 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
  12. Cannabinoid receptor 1 contributes to sprouted innervation in endometrial ectopic growth through mitogen-activated protein kinase activation.
    Authors: Han
    Brain Res  2017;1663:132
  13. 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
  14. 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
  15. Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells
    Authors: Mou Et al.
    Cell: Stem Cell  2016;19:217
  16. Pyrrolidine dithiocarbamate activates the Nrf2 pathway in astrocytes.
    Authors: Liddell Et al.
    J Neuroinflammation  2016;13:49
  17. Andrographolide induces Nrf2 and heme oxygenase 1 in astrocytes by activating p38 MAPK and ERK.
    Authors: Wong Et al.
    J Neuroinflammation  2016;13:251
  18. 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
  19. 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
  20. The LPA1/ZEB1/miR-21-activation pathway regulates metastasis in basal breast cancer.
    Authors: Sahay Et al.
    Int J Mol Med  2015;6:20604
  21. 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.
    Diabetologia  2015;58:2563
  22. Analysis of the anti-proliferative and the pro-apoptotic efficacy of Syk inhibition in multiple myeloma.
    Authors: Koerber Et al.
    Oncotarget  2015;4:21
  23. MAPK signaling downstream to TLR4 contributes to PacT.-induced peripheral neuropathy.
    Authors: Li Et al.
    Brain Behav.Immun.  2015;49:255
  24. MFG-E8 inhibits neutrophil migration through αvβ3-integrin-dependent MAP kinase activation.
    Authors: Aziz Et al.
    J Neuroinflammation  2015;36:18
  25. Different patterns of electrical activity lead to long-term potentiation by activating different intracellular pathways.
    Authors: Zhu Et al.
    PLoS One  2015;35:621
  26. 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
  27. Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.
    Authors: Lin Et al.
    Exp Hematol Oncol  2015;16:5555
  28. 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
  29. 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
  30. The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation.
    Authors: Smith Et al.
    Mol Cancer  2015;10:e0136546
  31. 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
  32. 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
  33. 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
  34. 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
  35. Oxytocin is an age-specific circulating hormone that is necessary for muscle maintenance and regeneration.
    Authors: Elabd Et al.
    Nat Commun  2014;5:4082
  36. Resolvin D2 supports MCF-7 cell proliferation via activation of estrogen receptor.
    Authors: Al-Zaubai Et al.
    J Pharmacol Exp Ther  2014;351:172
  37. 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
  38. 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
  39. 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
  40. 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
  41. BDNF-endocannabinoid interactions at neocortical inhibitory synapses require phospholipase C signaling.
    Authors: Zhao
    J Neurophysiol  2014;111:1008
  42. 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
  43. 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
  44. Group II metabotropic glutamate receptor agonist LY379268 regulates AMPA receptor trafficking in prefrontal cortical neurons.
    Authors: Wang Et al.
    Neuroscience  2013;8:e61787
  45. Effects of Y27632 on keratinocyte procurement and wound healing.
    Authors: Gandham Et al.
    PLoS One  2013;38:782
  46. 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
  47. 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
  48. Endocrine disruptors fludioxonil and fenhexamid stimulate miR-21 expression in breast cancer cells.
    Authors: Teng Et al.
    Toxicol Sci  2013;131:71
  49. 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;
  50. Ceramide 1-phosphate stimulates proliferation of C2C12 myoblasts.
    Authors: Gangoiti Et al.
    Biochimie  2012;94:597
  51. Inhibition of α-SMA by the ectodomain of FGFR2c attenuates lung fibrosis.
    Authors: Ju Et al.
    J Pharmacol Exp Ther  2012;18:992
  52. Curcumin inhibits glutamate release from rat prefrontal nerve endings by affecting vesicle mobilization.
    Authors: Lin Et al.
    J Biomed Sci  2012;13:9097
  53. 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
  54. A screen for regulators of survival of motor neuron protein levels.
    Authors: Makhortova Et al.
    Nat Chem Biol  2011;7:544
  55. Saccharomyces boulardii improves intestinal cell restitution through activation of the α2β1 integrin collagen receptor.
    Authors: Canonici Et al.
    Exp Cell Res  2011;6:e18427
  56. 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
  57. Reversible differentiation of myofibroblasts by MyoD.
    Authors: Hecker Et al.
    Br J Pharmacol  2011;317:1914
  58. 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
  59. Stanniocalcin-1 promotes tumor angiogenesis through up-regulation of VEGF in gastric cancer cells.
    Authors: He Et al.
    Mol Med  2011;18:39
  60. 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
  61. 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
  62. 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
  63. β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.
    Authors: Meitzen Et al.
    J Neurochem  2011;116:984
  64. 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
  65. Extranuclear estrogen receptors mediate the neuroprotective effects of estrogen in the rat hippocampus.
    Authors: Yang Et al.
    PLoS One  2010;5:e9851
  66. 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
  67. 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
  68. 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
  69. BC1 regulation of metabotropic glutamate receptor-mediated neuronal excitability.
    Authors: Zhong Et al.
    J Neurosci  2009;29:9977
  70. 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
  71. PLZF is a regulator of homeostatic and cytokine-induced myeloid development.
    Authors: Doulatov Et al.
    Genes Dev  2009;23:2076
  72. The kinase inhibitors suni. and sora. differentially affect NK cell antitumor reactivity in vitro.
    Authors: Krusch Et al.
    J Immunol  2009;183:8286
  73. 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
  74. Soy phytoestrogens are neuroprotective against stroke-like injury in vitro.
    Authors: Schreihofer and Redmond
    J Endocrinol  2009;158:602
  75. 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
  76. 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
  77. Mitogen-activated protein kinases mediate upregulation of hypothalamic angiotensin II type 1 receptors in heart failure rats.
    Authors: Wei Et al.
    Hypertension  2008;52:679
  78. 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.
    Carcinogenesis  2008;29:713
  79. 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
  80. 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
  81. Regulation of DA transporter function and cell surface expression by D3 DA receptors.
    Authors: Zapata Et al.
    J Biol Chem  2007;282:35842
  82. IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4.
    Authors: Chung Et al.
    J Endocrinol  2007;194:77
  83. Ins induces airway smooth muscle contraction.
    Authors: Schaafsma Et al.
    Int J Mol Sci  2007;150:136
  84. 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
  85. 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
  86. 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
  87. 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
  88. 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
  89. Ischemic preconditioning protects by activating prosurvival kinases at reperfusion.
    Authors: Hausenloy Et al.
    Am J Physiol Heart Circ Physiol  2005;288:H971
  90. Ob receptor in rabbit ovary and leptin in vitro regulation of corpora lutea.
    Authors: Zerani Et al.
    J Neuroinflammation  2004;183:279
  91. 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
  92. 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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PD 98059 abrogated the LPA induced phosphorylation of AMPK.
By lisha joshi on 06/18/2019
Species: Mouse

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 ERK pathway in LPA induced pro-inflammatory phenotype in microglia cells
By Joanna Plastira on 06/08/2019
Species: Mouse

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).


PD 98059 inhibits 15d-PGJ2 induced pp42/44 expression
By Chintan Koyani on 10/13/2018
Species: Mouse

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).


Inhibition of MEK in ovarian theca cells by PD98059
By Zhenmin Lei on 01/04/2018
Species: Mouse

Used to treat mouse ovarian theca cells to inhibit MEK and detected by Western blot.


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