PD 98059

Cat. No. 1213

PD 98059 C16H13NO3 [167869-21-8]

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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.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

Kojima et al (2007) Mitogen-activated protein kinase kinase inhibition enhances nuclear proapoptotic function of p53 in acute myelogenous leukemia cells. 67 3210. PMID: 17409429.

Qi et al (2004) BMP4 supports self-renewal of embryonic stem cells by inhibiting mitogen-activated protein kinase pathways. Proc.Natl.Acad.Sci.USA 101 6027. PMID: 15075392.

Tsang et al (1998) Effects of mitogen-activated protein kinase kinase inhibitor PD 98059 on antigen challenge of guinea-pig airways in vitro. Br.J.Pharmacol. 125 61. PMID: 9776345.

Alessi et al (1995) PD 98059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo. J.Biol.Chem. 270 27489. PMID: 7499206.

Dudley et al (1995) A synthetic inhibitor of the mitogen-activated protein kinase cascade. Proc.Natl.Acad.Sci.U.S.A. 92 7686. PMID: 7644477.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for PD 98059 include:

Edén et al (2015) Tissue factor/factor VIIa signalling promotes cytokine-induced beta cell death and impairs glucose-stimulated insulin secretion from human pancreatic islets. Diabetologia 58 2563. PMID: 26271343.

Feng et al (2015) Synergistic effects of high dietary calcium and exogenous parathyroid hormone in promoting osteoblastic bone formation in mice. Br J Nutr 113 909. PMID: 25744000.

Li et al (2015) MAPK signaling downstream to TLR4 contributes to paclitaxel-induced peripheral neuropathy. Brain Behav.Immun. 49 255. PMID: 26065826.

Tozzi et al (2015) Endogenous 17β-estradiol is required for activity-dependent long-term potentiation in the striatum: interaction with the dopaminergic system. Front Cell Neurosci 9 192. PMID: 26074768.

Al-Zaubai et al (2014) Resolvin D2 supports MCF-7 cell proliferation via activation of estrogen receptor. J Pharmacol Exp Ther 351 172. PMID: 25077525.

Elabd et al (2014) Oxytocin is an age-specific circulating hormone that is necessary for muscle maintenance and regeneration. Nat Commun 5 4082. PMID: 24915299.

Morelli et al (2014) Cross-talk between alpha1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation. BMC Cancer 14 921. PMID: 25481381.

Sizemore et al (2014) GABA(A) receptor pi (GABRP) stimulates basal-like breast cancer cell migration through activation of extracellular-regulated kinase 1/2 (ERK1/2). J Biol Chem 289 24102. PMID: 25012653.

Yu et al (2014) Differential effects of the Toll-like receptor 2 agonists, PGN and Pam3CSK4 on anti-IgE induced human mast cell activation. PLoS One 9 e112989. PMID: 25398056.

Ahmadiantehrani and Ron (2013) Dopamine D2 receptor activation leads to an up-regulation of glial cell line-derived neurotrophic factor via Gβγ-Erk1/2-dependent induction of Zif268. J Neurochem. PMID: 23373701.

Akhtar et al (2013) Activation of ErbB2 and Downstream Signalling via Rho Kinases and ERK1/2 Contributes to Diabetes-Induced Vascular Dysfunction. PLoS One 8 e67813. PMID: 23826343.

Kim et al (2013) Epigallocatechin gallate (EGCG) stimulates autophagy in vascular endothelial cells: a potential role for reducing lipid accumulation. J Biol Chem 288 22693. PMID: 23754277.

Teng et al (2013) Endocrine disruptors fludioxonil and fenhexamid stimulate miR-21 expression in breast cancer cells. Toxicol Sci 131 71. PMID: 23052036.

Gangoiti et al (2012) Ceramide 1-phosphate stimulates proliferation of C2C12 myoblasts. Biochimie 94 597. PMID: 21945811.

Barrio et al (2011) Neurotoxicity induced by okadaic acid in the human neuroblastoma SH-SY5Y line can be differentially prevented by α7 and β2* nicotinic stimulation. Toxicol Sci 123 193. PMID: 21715663.

Jung et al (2011) IL-32gamma induces the maturation of dendritic cells with Th1- and Th17-polarizing ability through enhanced IL-12 and IL-6 production. J Immunol 186 6848. PMID: 21551364.

Kloster et al (2011) Hyperactivation of NF-κB via the MEK signaling is indispensable for the inhibitory effect of cAMP on DNA damage-induced cell death. Mol Cancer 10 45. PMID: 21510868.

Meitzen et al (2011) β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons. J Neurochem 116 984. PMID: 21143600.

Mockett et al (2011) Calcium/calmodulin-dependent protein kinase II mediates group I metabotropic glutamate receptor-dependent protein synthesis and long-term depression in rat hippocampus. J Neurosci 31 7380. PMID: 21593322.

Roselli et al (2009) Disassembly of shank and homer synaptic clusters is driven by soluble beta-amyloid(1-40) through divergent NMDAR-dependent signalling pathways. PLoS One 4 e6011. PMID: 19547699.

Yeligar et al (2009) 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. J Immunol 183 5964. PMID: 19828633.

Zhong et al (2009) BC1 regulation of metabotropic glutamate receptor-mediated neuronal excitability. J Neurosci 29 9977. PMID: 19675232.

Jung et al (2008) 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. Carcinogenesis 29 713. PMID: 18258605.

Kim et al (2008) Inhibition of AMP-activated protein kinase sensitizes cancer cells to cisplatin-induced apoptosis via hyper-induction of p53. J Biol Chem 283 3731. PMID: 18079115.

Chung et al (2007) IGF-I inhibition of apoptosis is associated with decreased expression of prostate apoptosis response-4. J Endocrinol 194 77. PMID: 17592023.

Lin et al (2007) GSK-3beta acts downstream of PP2A and the PI 3-kinase-Akt pathway, and upstream of caspase-2 in ceramide-induced mitochondrial apoptosis. J Cell Sci 120 2935. PMID: 17666435.

Zapata et al (2007) Regulation of dopamine transporter function and cell surface expression by D3 dopamine receptors. J Biol Chem 282 35842. PMID: 17923483.

Kauppinen et al (2006) Direct phosphorylation and regulation of poly(ADP-ribose) polymerase-1 by extracellular signal-regulated kinases 1/2. Proc Natl Acad Sci U S A 103 7136. PMID: 16627622.

Sarfaraz et al (2006) Cannabinoid receptor agonist-induced apoptosis of human prostate cancer cells LNCaP proceeds through sustained activation of ERK1/2 leading to G1 cell cycle arrest. J Biol Chem 281 39480. PMID: 17068343.

Sunters et al (2006) Paclitaxel-induced nuclear translocation of FOXO3a in breast cancer cells is mediated by c-Jun NH2-terminal kinase and Akt. Cancer Res 66 212. PMID: 16397234.

Alonso-Magdalena et al Pancreatic insulin content regulation by the estrogen receptor ER alpha. PLoS One 3 e2069. PMID: 18446233.

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Keywords: PD 98059, supplier, Specific, inhibitors, MEK, MKK, Mitogen-Activated, Protein, Kinase, Kinases, PD98059, stem, cells, Tocris Bioscience, MEK Inhibitor products

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