PD 98059

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Cat.No. 1213 - PD 98059 | C16H13NO3 | CAS No. 167869-21-8
Description: MEK inhibitor
Chemical Name: 2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one
Purity: ≥98% (HPLC)
Datasheet
Citations (83)
Reviews (1)
Literature
Pathways

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™.

Compound Libraries

PD 98059 is also offered as part of the Tocriscreen Plus, Tocriscreen Kinase Inhibitor Toolbox I and Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 267.28
Formula C16H13NO3
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 167869-21-8
PubChem ID 9794588
InChI Key PKDHDJBNEKXCBI-UHFFFAOYSA-N
Smiles COC1=C(N)C(=CC=C1)C1=CC(=O)C2=CC=CC=C2O1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 6.68 25
ethanol 1.34 5

Preparing Stock Solutions

The following data is based on the product molecular weight 267.28. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.74 mL 18.71 mL 37.41 mL
5 mM 0.75 mL 3.74 mL 7.48 mL
10 mM 0.37 mL 1.87 mL 3.74 mL
50 mM 0.07 mL 0.37 mL 0.75 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the biological activity of the product.

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

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

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

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


If you know of a relevant reference for PD 98059, please let us know.

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Keywords: PD 98059, PD 98059 supplier, Specific, inhibitors, inhibits, MEK, MKK, Mitogen-Activated, Protein, Kinase, Kinases, PD98059, stem, cells, Stem, Cell, Proliferation, 1213, Tocris Bioscience

83 Citations for PD 98059

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

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

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

Zhao (2014) BDNF-endocannabinoid interactions at neocortical inhibitory synapses require phospholipase C signaling. J Neurophysiol 111 1008 PMID: 24335212

Yuen et al (2014) Synergistic regulation of glutamatergic transmission by serotonin and norepinephrine reuptake inhibitors in prefrontal cortical neurons. J Biol Chem 289 25177 PMID: 25056951

Kook et al (2013) Fibroblast growth factor-4 enhances proliferation of mouse embryonic stem cells via activation of c-Jun signaling. PLoS One 8 e71641 PMID: 23967228

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

Yang et al (2010) Extranuclear estrogen receptors mediate the neuroprotective effects of estrogen in the rat hippocampus. PLoS One 5 e9851 PMID: 20479872

Wong et al (2010) Bone morphogenic protein-4 impairs endothelial function through oxidative stress-dependent cyclooxygenase-2 upregulation: implications on hypertension. Circ Res 107 984 PMID: 20724703

Huang et al (2010) Pharmacological and genetic accumulation of hypoxia-inducible factor-1alpha enhances excitatory synaptic transmission in hippocampal neurons through the production of vascular endothelial growth factor. J Neurosci 30 6080 PMID: 20427666

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

Li et al (2017) Follicular Stimulating Hormone Accelerates Atherogenesis by Increasing Endothelial VCAM-1 Expression. Theranostics 7 4671 PMID: 29187895

Inda et al (2017) cAMP-dependent cell differentiation triggered by activated CRHR1 in hippocampal neuronal cells. Sci Rep 7 1944 PMID: 28512295

Rao and Herr (2017) G protein-coupled receptor GPR19 regulates E-cadherin expression and invasion of breast cancer cells Biochim Biophys Acta 1864 1318 PMID: 28476646

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

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

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

Fernández-Pisonero et al (2014) Synergy between sphingosine 1-phosphate and lipopolysaccharide signaling promotes an inflammatory, angiogenic and osteogenic response in human aortic valve interstitial cells. PLoS One 9 e109081 PMID: 25275309

Beermann et al (2014) Distinct signalling pathways of murine histamine H1- and H4-receptors expressed at comparable levels in HEK293 cells. PLoS One 9 e107481 PMID: 25243776

Suk et al (2013) A Taiwanese Propolis Derivative Induces Apoptosis through Inducing Endoplasmic Reticular Stress and Activating Transcription Factor-3 in Human Hepatoma Cells. Evid Based Complement Alternat Med 2013 658370 PMID: 24222778

Sutcliffe et al (2009) Transcriptional regulation of monocyte chemotactic protein-1 release by endothelin-1 in human airway smooth muscle cells involves NF-kappaB and AP-1. Br J Pharmacol 157 436 PMID: 19371341

Schaafsma et al (2007) Insulin induces airway smooth muscle contraction. Int J Mol Sci 150 136 PMID: 17160007

Alao et al (2006) 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. J Biol Chem 5 40 PMID: 17018141

Han (2017) Cannabinoid receptor 1 contributes to sprouted innervation in endometrial ectopic growth through mitogen-activated protein kinase activation. Brain Res 1663 132 PMID: 28322749

Makhortova et al (2011) A screen for regulators of survival of motor neuron protein levels. Nat Chem Biol 7 544 PMID: 21685895

Cho et al (2009) Synergistic effect of ERK inhibition on tetrandrine-induced apoptosis in A549 human lung carcinoma cells. J Vet Sci 10 23 PMID: 19255520

Krusch et al (2009) The kinase inhibitors sunitinib and sorafenib differentially affect NK cell antitumor reactivity in vitro. J Immunol 183 8286 PMID: 20007592

Doulatov et al (2009) PLZF is a regulator of homeostatic and cytokine-induced myeloid development. Genes Dev 23 2076 PMID: 19723763

Roozendaal et al (2009) Glucocorticoid effects on memory consolidation depend on functional interactions between the medial prefrontal cortex and basolateral amygdala. J Neurosci 29 14299 PMID: 19906977

Schreihofer and Redmond (2009) Soy phytoestrogens are neuroprotective against stroke-like injury in vitro. J Endocrinol 158 602 PMID: 18976694

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

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

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

Hausenloy et al (2005) Ischemic preconditioning protects by activating prosurvival kinases at reperfusion. Am J Physiol Heart Circ Physiol 288 H971 PMID: 15358610

Mou et al (2016) Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells Cell: Stem Cell 19 217 PMID: 27320041

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

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

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

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

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

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

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

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

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

Tsai et al (2011) 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. J Nutr 141 2119 PMID: 22031657

Olianas et al (2016) The GABAB positive allosteric modulators CGP7930 and GS39783 stimulate ERK1/2 signalling in cellslacking functional GABAB receptors European Journal of Pharmacology 794 135 PMID: 27876620

Rahman et al (2016) 18α-glycyrrhetinic acid lethality for neuroblastoma cells via de-regulating the Beclin-1/Bcl-2 complex and inducing apoptosis. Biochemical Pharmacology 117 97 PMID: 27520483

Gudasheva et al (2015) Dimeric dipeptide mimetics of the nerve growth factor Loop 4 and Loop 1 activate TRKA with different patterns of intracellular signal transduction. Int J Mol Sci 22 106 PMID: 26642930

Lin et al (2015) Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals. Exp Hematol Oncol 16 5555 PMID: 25768340

Koerber et al (2015) Analysis of the anti-proliferative and the pro-apoptotic efficacy of Syk inhibition in multiple myeloma. Oncotarget 4 21 PMID: 26251761

Sahay et al (2015) The LPA1/ZEB1/miR-21-activation pathway regulates metastasis in basal breast cancer. Int J Mol Med 6 20604 PMID: 26098771

Aziz et al (2015) MFG-E8 inhibits neutrophil migration through αvβ3-integrin-dependent MAP kinase activation. J Neuroinflammation 36 18 PMID: 25936372

Vuong et al (2015) NF-κB transcriptional activation by TNFα requires phospholipase C, extracellular signal-regulated kinase 2 and poly(ADP-ribose) polymerase-1. J Neurosci 12 229 PMID: 26637332

Zhu et al (2015) Different patterns of electrical activity lead to long-term potentiation by activating different intracellular pathways. PLoS One 35 621 PMID: 25589756

Smith et al (2015) The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation. Mol Cancer 10 e0136546 PMID: 26414859

Gonsalves et al (2014) Angiogenic growth factors augment K-Cl cotransporter expression in erythroid cells via hypoxia-inducible factor-1α. Am J Hematol 89 273 PMID: 24227191

Wei et al (2014) Central SDF-1/CXCL12 expression and its cardiovascular and sympathetic effects: the role of angiotensin II, TNF-α, and MAP kinase signaling. Am J Physiol Heart Circ Physiol 307 H1643 PMID: 25260613

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

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

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

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

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

Zerani et al (2004) Ob receptor in rabbit ovary and leptin in vitro regulation of corpora lutea. J Neuroinflammation 183 279 PMID: 15531716

Wong et al (2016) Andrographolide induces Nrf2 and heme oxygenase 1 in astrocytes by activating p38 MAPK and ERK. J Neuroinflammation 13 251 PMID: 27663973

Gandham et al (2013) Effects of Y27632 on keratinocyte procurement and wound healing. PLoS One 38 782 PMID: 23675999

Wang et al (2013) Group II metabotropic glutamate receptor agonist LY379268 regulates AMPA receptor trafficking in prefrontal cortical neurons. Neuroscience 8 e61787 PMID: 23593498

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

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

Atherton et al (2003) IL-13-induced changes in the goblet cell density of human bronchial epithelial cell cultures: MAP kinase and phosphatidylinositol 3-kinase regulation. Am J Physiol Lung Cell Mol Physiol 285 L730 PMID: 12794003

Martin et al (2003) Delphinidin, an active compound of red wine, inhibits endothelial cell apoptosis via nitric oxide pathway and regulation of calcium homeostasis. Br J Pharmacol 139 1095 PMID: 12871827

Lin et al (2012) Curcumin inhibits glutamate release from rat prefrontal nerve endings by affecting vesicle mobilization. J Biomed Sci 13 9097 PMID: 22942754

Ju et al (2012) Inhibition of α-SMA by the ectodomain of FGFR2c attenuates lung fibrosis. J Pharmacol Exp Ther 18 992 PMID: 22451267

He et al (2011) Stanniocalcin-1 promotes tumor angiogenesis through up-regulation of VEGF in gastric cancer cells. Mol Med 18 39 PMID: 21672207

Canonici et al (2011) Saccharomyces boulardii improves intestinal cell restitution through activation of the α2β1 integrin collagen receptor. Exp Cell Res 6 e18427 PMID: 21483797

Hecker et al (2011) Reversible differentiation of myofibroblasts by MyoD. Br J Pharmacol 317 1914 PMID: 21440539

Yoon et al (2011) Wnt5a-dopamine D2 receptor interactions regulate dopamine neuron development via extracellular signal-regulated kinase (ERK) activation. PLoS One 286 15641 PMID: 21454669

Kovac et al (2011) Brain microvascular pericytes are immunoactive in culture: cytokine, chemokine, nitric oxide, and LRP-1 expression in response to lipopolysaccharide. J Biomed Sci 8 139 PMID: 21995440

Kim et al (2008) Differential enhancement of leukaemia cell differentiation without elevation of intracellular calcium by plant-derived sesquiterpene lactone compounds. Br J Pharmacol 155 814 PMID: 18724384

Wei et al (2008) Mitogen-activated protein kinases mediate upregulation of hypothalamic angiotensin II type 1 receptors in heart failure rats. Hypertension 52 679 PMID: 18768402


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Inhibition of MEK in ovarian theca cells by PD98059
By Zhenmin Lei on 01/04/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Ovarian theca cells

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


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MAPK Signaling Scientific Review

MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.

Pathways for PD 98059

MAPK

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.