Catalog Number: 1213
Chemical Name: 2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one
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. All Tocris products are intended for laboratory research use only.
Background References
  1. Mitogen-activated protein kinase kinase inhibition enhances nuclear proapoptotic function of p53 in acute myelogenous leukemia cells.
    Kojima K, Konopleva M, Samudio IJ et al.
    Cancer Res.
  2. PD 98059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo.
    Alessi et al.
    J.Biol.Chem., 1995;270:27489
  3. A synthetic inhibitor of the mitogen-activated protein kinase cascade.
    Dudley et al.
    Proc.Natl.Acad.Sci.U.S.A., 1995;92:7686
  4. Effects of mitogen-activated protein kinase kinase inhibitor PD 98059 on antigen challenge of guinea-pig airways in vitro.
    Tsang et al.
    Br.J.Pharmacol., 1998;125:61
  5. BMP4 supports self-renewal of embryonic stem cells by inhibiting mitogen-activated protein kinase pathways.
    Qi et al.
    Proc.Natl.Acad.Sci.USA, 2004;101:6027
Citations:

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

59 Citations: Showing 1 - 10
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  1. Pancreatic insulin content regulation by the estrogen receptor ER alpha.
    Authors: Alonso-Magdalena Et al.
    PLoS One ;3:e2069
  2. 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
  3. Cannabinoid receptor 1 contributes to sprouted innervation in endometrial ectopic growth through mitogen-activated protein kinase activation.
    Authors: Han
    Brain Res 2017;1663:132
  4. 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
  5. Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells
    Authors: Mou Et al.
    Cell: Stem Cell 2016;19:217
  6. 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
  7. 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
  8. The LPA1/ZEB1/miR-21-activation pathway regulates metastasis in basal breast cancer.
    Authors: Sahay Et al.
    Int J Mol Med 2015;6:20604
  9. 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.
    Diabetologia 2015;58:2563
  10. Analysis of the anti-proliferative and the pro-apoptotic efficacy of Syk inhibition in multiple myeloma.
    Authors: Koerber Et al.
    Oncotarget 2015;4:21
  11. MAPK signaling downstream to TLR4 contributes to paclitaxel-induced peripheral neuropathy.
    Authors: Li Et al.
    Brain Behav.Immun. 2015;49:255
  12. MFG-E8 inhibits neutrophil migration through αvβ3-integrin-dependent MAP kinase activation.
    Authors: Aziz Et al.
    J Neuroinflammation 2015;36:18
  13. Different patterns of electrical activity lead to long-term potentiation by activating different intracellular pathways.
    Authors: Zhu Et al.
    PLoS One 2015;35:621
  14. 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
  15. Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.
    Authors: Lin Et al.
    Exp Hematol Oncol 2015;16:5555
  16. 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
  17. 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
  18. The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation.
    Authors: Smith Et al.
    Mol Cancer 2015;10:e0136546
  19. 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
  20. 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
  21. 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
  22. Oxytocin is an age-specific circulating hormone that is necessary for muscle maintenance and regeneration.
    Authors: Elabd Et al.
    Nat Commun 2014;5:4082
  23. Resolvin D2 supports MCF-7 cell proliferation via activation of estrogen receptor.
    Authors: Al-Zaubai Et al.
    J Pharmacol Exp Ther 2014;351:172
  24. 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
  25. 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
  26. 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
  27. Group II metabotropic glutamate receptor agonist LY379268 regulates AMPA receptor trafficking in prefrontal cortical neurons.
    Authors: Wang Et al.
    Neuroscience 2013;8:e61787
  28. Effects of Y27632 on keratinocyte procurement and wound healing.
    Authors: Gandham Et al.
    PLoS One 2013;38:782
  29. 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
  30. Endocrine disruptors fludioxonil and fenhexamid stimulate miR-21 expression in breast cancer cells.
    Authors: Teng Et al.
    Toxicol Sci 2013;131:71
  31. 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;
  32. Ceramide 1-phosphate stimulates proliferation of C2C12 myoblasts.
    Authors: Gangoiti Et al.
    Biochimie 2012;94:597
  33. Inhibition of α-SMA by the ectodomain of FGFR2c attenuates lung fibrosis.
    Authors: Ju Et al.
    J Pharmacol Exp Ther 2012;18:992
  34. Curcumin inhibits glutamate release from rat prefrontal nerve endings by affecting vesicle mobilization.
    Authors: Lin Et al.
    J Biomed Sci 2012;13:9097
  35. 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
  36. Saccharomyces boulardii improves intestinal cell restitution through activation of the α2β1 integrin collagen receptor.
    Authors: Canonici Et al.
    Exp Cell Res 2011;6:e18427
  37. 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
  38. Reversible differentiation of myofibroblasts by MyoD.
    Authors: Hecker Et al.
    Br J Pharmacol 2011;317:1914
  39. 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
  40. Stanniocalcin-1 promotes tumor angiogenesis through up-regulation of VEGF in gastric cancer cells.
    Authors: He Et al.
    Mol Med 2011;18:39
  41. 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
  42. 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
  43. β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.
    Authors: Meitzen Et al.
    J Neurochem 2011;116:984
  44. 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
  45. 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
  46. BC1 regulation of metabotropic glutamate receptor-mediated neuronal excitability.
    Authors: Zhong Et al.
    J Neurosci 2009;29:9977
  47. 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
  48. Soy phytoestrogens are neuroprotective against stroke-like injury in vitro.
    Authors: Schreihofer and Redmond
    J Endocrinol 2009;158:602
  49. 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
  50. 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
  51. Regulation of dopamine transporter function and cell surface expression by D3 dopamine receptors.
    Authors: Zapata Et al.
    J Biol Chem 2007;282:35842
  52. IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4.
    Authors: Chung Et al.
    J Endocrinol 2007;194:77
  53. Insulin induces airway smooth muscle contraction.
    Authors: Schaafsma Et al.
    Int J Mol Sci 2007;150:136
  54. 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
  55. 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
  56. 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
  57. 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
  58. 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
  59. Ob receptor in rabbit ovary and leptin in vitro regulation of corpora lutea.
    Authors: Zerani Et al.
    J Neuroinflammation 2004;183:279
Expand to show all 59 Citations

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