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Submit ReviewPD 98059
说明： MEK inhibitor
化学名： 2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one
纯度： ≥98% (HPLC)
生物活性 for PD 98059
PD 98059 is an 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.
化合物库 for PD 98059
PD 98059 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library, Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library. 了解 Tocris 化合物库的更多信息。
技术数据 for PD 98059
| 分子量 | 267.28 |
| 公式 | C16H13NO3 |
| 储存 | Store at RT |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for PD 98059
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 6.68 | 25 | |
| ethanol | 1.34 | 5 |
制备储备液 for PD 98059
以下数据基于产品分子量 267.28。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.25 mM | 14.97 mL | 74.83 mL | 149.66 mL |
| 1.25 mM | 2.99 mL | 14.97 mL | 29.93 mL |
| 2.5 mM | 1.5 mL | 7.48 mL | 14.97 mL |
| 12.5 mM | 0.3 mL | 1.5 mL | 2.99 mL |
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产品说明书 for PD 98059
参考文献 for PD 98059
参考文献是支持产品生物活性的出版物。
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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关键词: PD 98059, PD 98059 supplier, Specific, inhibitors, inhibits, MEK, MKK, Mitogen-Activated, Protein, Kinase, Kinases, PD98059, stem, cells, Stem, Cell, Proliferation, 1213, Tocris Bioscience
96 篇 PD 98059 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PD 98059 的部分引用包括：
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
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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
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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
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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
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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
Yoon et al (2011) Wnt5a-DA D2 receptor interactions regulate DA neuron development via extracellular signal-regulated kinase (ERK) activation. PLoS One 286 15641 PMID: 21454669
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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
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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
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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
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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
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Kim et al (2019) LRRK2 kinase plays a critical role in manganese-induced inflammation and apoptosis in microglia. PLoS One 14 e0210248 PMID: 30645642
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Liang et al (2017) Six-transmembrane epithelial antigens of the prostate comprise a novel inflammatory nexus in patients with pustular skin disorders. J Allergy Clin Immunol 139 1217 PMID: 27884600
Echeverría et al (2019) The sensitivity to Hsp90 inhibitors of both normal and oncogenically transformed cells is determined by the equilibrium between cellular quiescence and activity. PLoS One 14 e0208287 PMID: 30726209
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
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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) DA 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
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
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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
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
Li et al (2015) MAPK signaling downstream to TLR4 contributes to PacT.-induced peripheral neuropathy. Brain Behav.Immun. 49 255 PMID: 26065826
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
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
Krusch et al (2009) The kinase inhibitors suni. and sora. differentially affect NK cell antitumor reactivity in vitro. J Immunol 183 8286 PMID: 20007592
Schreihofer and Redmond (2009) Soy phytoestrogens are neuroprotective against stroke-like injury in vitro. J Endocrinol 158 602 PMID: 18976694
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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
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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
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PD 98059 treatment.
By
Xiaoyu Zhang on 02/07/2024
分析类型： In Vitro
种属： Mouse
细胞系/组织： neuron cells
Cultured mouse neuron treated with PD 98059 (10uM) for 15 mins. MAP staining showed after treatment.
PD 98059 abrogated the LPA induced phosphorylation of AMPK..
By
lisha joshi on 06/18/2019
分析类型： In Vitro
种属： Mouse
细胞系/组织： BV2 microglia cells
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
分析类型： In Vitro
种属： Mouse
细胞系/组织： Primary murine microglia cells
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
分析类型： In Vitro
种属： Mouse
细胞系/组织： HL-1 cardiomyocytes
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
分析类型： In Vitro
种属： Mouse
细胞系/组织： Ovarian theca cells
Used to treat mouse ovarian theca cells to inhibit MEK and detected by Western blot.
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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
