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说明： Potent, selective inhibitor of MEK1 and 2
化学名： 1,4-Diamino-2,3-dicyano-1,4-bis[2-aminophenylthio]butadiene
生物活性 for U0126
U0126 is a potent and selective non-competitive inhibitor of MAP kinase kinase. Inhibits MEK-1 and MEK-2 (IC50 values of 0.07 and 0.06 μM respectively) with little or no effect on the activities of PKC, Abl, Raf, MEKK, ERK, JNK, MKK-3, MKK-4/SEK, MKK-6, Cdk2 or Cdk4. Brain penetrant. Helps maintain human pluripotent stem cells in undifferentiated state.
Negative Control also available.
技术数据 for U0126
| 分子量 | 380.48 |
| 公式 | C18H16N6S2 |
| 储存 | Desiccate at +4°C |
| CAS Number | 109511-58-2 |
| PubChem ID | 3006531 |
| InChI Key | DVEXZJFMOKTQEZ-JYFOCSDGSA-N |
| Smiles | N\C(SC1=CC=CC=C1N)=C(C#N)/C(C#N)=C(\N)SC1=CC=CC=C1N |
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 U0126
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 38.05 | 100 |
制备储备液 for U0126
以下数据基于产品分子量 380.48。 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 |
|---|---|---|---|
| 1 mM | 2.63 mL | 13.14 mL | 26.28 mL |
| 5 mM | 0.53 mL | 2.63 mL | 5.26 mL |
| 10 mM | 0.26 mL | 1.31 mL | 2.63 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
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产品说明书 for U0126
参考文献 for U0126
参考文献是支持产品生物活性的出版物。
Davies et al (2000) Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem.J. 351 95 PMID: 10998351
Duncia et al (1998) MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products. Bioorg.Med.Chem.Lett. 8 2839 PMID: 9873633
Favata et al (1998) Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J.Biol.Chem. 273 18623 PMID: 9660836
Namura et al (2001) Intravenous administraton of MEK inhibitor U0126 affords brain protection against forebrain ischemia and focal cerebral ischemia. Proc.Natl.Acad.Sci.U.S.A. 98 11569 PMID: 11504919
Kinehara et al (2013) Protein kinase C regulates human pluripotent stem cell self-renewal. PLoS One 8 e54122 PMID: 23349801
If you know of a relevant reference for U0126, please let us know.
按产品操作查看相关产品
关键词: U0126, U0126 supplier, Potent, selective, inhibitors, inhibits, MEK1, MEK2, Mitogen-Activated, Protein, Kinase, Kinases, MEK, Stem, Cell, Proliferation, 1144, Tocris Bioscience
131 篇 U0126 的引用文献
引用文献是使用了 Tocris 产品的出版物。 U0126 的部分引用包括：
Collar et al (2018) The homozygous CX3CR1-M280 mutation impairs human monocyte survival. JCI Insight 3 e95417 PMID: 29415879
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Dohgu et al (2011) Lipopolysaccharide-enhanced transcellular transport of HIV-1 across the blood-brain barrier is mediated by luminal microvessel IL-6 and GM-CSF. Br J Pharmacol 8 167 PMID: 22129063
Hsu et al (2011) JNK suppression is essential for 17β-OE inhibits prostaglandin E2-Induced uPA and MMP-9 expressions and cell migration in human LoVo colon cancer cells. Cell Commun Signal 18 61 PMID: 21859479
Mou et al (2011) Rapid brain-derived neurotrophic factor-dependent sequestration of amygdala and hippocampal GABA(A) receptors via different tyrosine receptor kinase B-mediated phosphorylation pathways. Respir Res 176 72 PMID: 21195749
Kim et al (2011) Thrombin-induced Migration and Matrix Metalloproteinase-9 Expression Are Regulated by MAPK and PI3K Pathways in C6 Glioma Cells. Mol Cancer 15 211 PMID: 21994479
Kovac et al (2011) Brain microvascular pericytes are immunoactive in culture: cytokine, chemokine, nitric oxide, and LRP-1 expression in response to lipopolysaccharide. J Neurosci 8 139 PMID: 21995440
Zhang et al (2016) Bromodomain containing protein represses the Ras/Raf/MEK/ERK pathway to attenuate human hepatoma cell proliferation during HCV infection. Cancer Lett. 371 107 PMID: 26620707
Lourenco et al (2015) Macrophage migration inhibitory factor-CXCR4 is the dominant chemotactic axis in human mesenchymal stem cell recruitment to tumors. J Immunol 194 3463 PMID: 25712213
Tang et al (2015) P2X7 Receptor Regulates Internalization of Antimicrobial Peptide LL-37 by Human Macrophages That Promotes Intracellular Pathogen Clearance. J Immunol 195 1191 PMID: 26116509
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Melemedjian et al (2011) Targeting adenosine monophosphate-activated protein kinase (AMPK) in preclinical models reveals a potential mechanism for the treatment of neuropathic pain. Mol Pain 7 70 PMID: 21936900
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Gillman et al (2017) Epidermal Growth Factor Receptor Signaling Enhances the Proinflammatory Effects of Staphylococcus aureus Gamma-Toxin on the Mucosa. Toxins (Basel) 9 202 PMID: 28657583
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Cagnetta et al (2019) Noncanonical Modulation of the eIF2 Pathway Controls an Increase in Local Translation during Neural Wiring. Mol Cell 73 474 PMID: 30595434
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Alpár et al (2014) Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling. Cell Rep 5 4421 PMID: 25030704
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Li et al (2013) Effect of VIP on intracellular [Ca2+], extracellular regulated kinase 1/2, and secretion in cultured rat conjunctival goblet cells. Invest Ophthalmol Vis Sci 54 2872 PMID: 23518767
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 125 193 PMID: 23373701
Ripple et al (2013) Acute mitochondrial inhibition by mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK) 1/2 inhibitors regulates proliferation. J Biol Chem 288 2933 PMID: 23235157
Osgood et al (2013) Polycyclic aromatic hydrocarbon-induced signaling events relevant to inflammation and tumorigenesis in lung cells are dependent on molecular structure. PLoS One 8 e65150 PMID: 23755184
Korb et al (2013) Arc in the nucleus regulates PML-dependent GluA1 transcription and homeostatic plasticity. Nat Neurosci 16 874 PMID: 23749147
Lucchetti et al (2013) The prolyl isomerase Pin1 acts synergistically with CDK2 to regulate the basal activity of estrogen receptor α in breast cancer. PLoS One 8 e55355 PMID: 23390529
Melemedjian et al (2013) mTORC1 inhibition induces pain via IRS-1-dependent feedback activation of ERK. Pain 154 1080 PMID: 23607966
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Morse et al (2011) Ligand-directed functional selectivity at the mu opioid receptor revealed by label-free integrative pharmacology on-target. PLoS One 6 e25643 PMID: 22003401
Tsuda et al (2009) Mechanisms underlying fibronectin-induced up-regulation of P2X4R expression in microglia: distinct roles of PI3K-Akt and MEK-ERK signalling pathways. J Cell Mol Med 13 3251 PMID: 19298529
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
Roscioni et al (2009) PKA and Epac cooperate to augment bradykinin-induced interleukin-8 release from human airway smooth muscle cells. Respir Res 10 88 PMID: 19788733
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Pintchovski et al (2009) The serum response factor and a putative novel transcription factor regulate expression of the immediate-early gene Arc/Arg3.1 in neurons. J Neurosci 29 1525 PMID: 19193899
Magliaro and Saldanha (2009) Clozapine protects PC-12 cells from death due to oxidative stress induced by hydrogen peroxide via a cell-type specific mechanism involving inhibition of extracellular signal-regulated kinase phosphorylation. Brain Res 1283 14 PMID: 19501068
Riedl et al (2009) Proteomic analysis uncovers novel actions of the neurosecretory protein VGF in nociceptive processing. PLoS One 29 13377 PMID: 19846725
Devocelle et al (2019) Inhibition of TGF-β1 Signaling by IL-15: A Novel Role for IL-15 in the Control of Renal Epithelial-Mesenchymal Transition: IL-15 Counteracts TGF-β1-Induced EMT in Renal Fibrosis. Int J Cell Biol 2019 9151394 PMID: 31360169
Zhen et al (2019) Purpurogallin Protects Keratinocytes from Damage and Apoptosis Induced by Ultraviolet B Radiation and Particulate Matter 2.5. Biomol Ther (Seoul) 27 395 PMID: 30419635
Suo et al (2019) Inhibition of MAPK/ERK pathway promotes oligodendrocytes generation and recovery of demyelinating diseases. Glia 67 1320 PMID: 30815939
Wan and Goldman (2017) Opposing Actions of Fgf8a on Notch Signaling Distinguish Two Muller Glial Cell Populations that Contribute to Retina Growth and Regeneration. Cell Rep 19 849 PMID: 28445734
Wu (2017) TRIB3 downregulation enhances doxorubicin-induced cytotoxicity in gastric cancer cells. Arch Biochem Biophys 622 26 PMID: 28442401
Saliba et al (2015) Evidence of a Role for Fibroblast Transient Receptor Potential Canonical 3 Ca2+ Channel in Renal Fibrosis. J Am Soc Nephrol 26 1855 PMID: 25479966
Li et al (2015) MAPK signaling downstream to TLR4 contributes to PacT.-induced peripheral neuropathy. Brain Behav.Immun. 49 255 PMID: 26065826
Zhang et al (2012) Activation of the Ras/Raf/MEK pathway facilitates hepatitis C virus replication via attenuation of the IF.-JAK-STAT pathway. J Virol 86 1544 PMID: 22114332
Chen et al (2012) Curcumin inhibits HCV replication by induction of heme oxygenase-1 and suppression of AKT. Int J Mol Med 30 1021 PMID: 22922731
Upham et al (2009) Structure-activity-dependent regulation of cell communication by perfluorinated fatty acids using in vivo and in vitro model systems. Environ Health Perspect 117 545 PMID: 19440492
Doulatov et al (2009) PLZF is a regulator of homeostatic and cytokine-induced myeloid development. Genes Dev 23 2076 PMID: 19723763
Park et al (2009) 4-hydroxyOE induces anchorage-independent growth of human mammary epithelial cells via activation of IkappaB kinase: potential role of reactive oxygen species. Cancer Res 69 2416 PMID: 19276383
Pietak et al (2019) Neural control of body-plan axis in regenerating planaria. PLoS Comput Biol 15 e1006904 PMID: 30990801
Szybowska et al (2019) Cancer Mutations in FGFR2 Prevent a Negative Feedback Loop Mediated by the ERK1/2 Pathway. Cells 8 518 PMID: 31146385
Wang et al (2016) Corticotrigeminal Projections from the Insular Cortex to the Trigeminal Caudal Subnucleus Regulate Orofacial Pain after Nerve Injury via Extracellular Signal-Regulated Kinase Activation in Insular Cortex Neurons. Front Cell Neurosci 9 493 PMID: 26733817
Berdichevsky et al (2013) PI3K-Akt signaling activates mTOR-mediated epileptogenesis in organotypic hippocampal culture model of post-traumatic epilepsy. J Neurosci 33 9056 PMID: 23699517
Yan et al (2012) Sensitization of dural afferents underlies migraine-related behavior following meningeal application of interleukin-6 (IL-6). Mol Pain 8 6 PMID: 22273495
Li et al (2012) Hepatitis C virus activates Bcl-2 and MMP-2 expression through multiple cellular signaling pathways. J Virol 86 12531 PMID: 22951829
Ye et al (2012) Local synaptic integration of mitogen-activated protein kinase and protein kinase A signaling mediates intermediate-term synaptic facilitation in Aplysia. Proc Natl Acad Sci U S A 109 18162 PMID: 23071303
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
Huang and Hsu (2010) Activation of muscarinic acetylcholine receptors induces a nitric oxide-dependent long-term depression in rat medial prefrontal cortex. Cereb Cortex 20 982 PMID: 19666830
Chen et al (2010) Ca(v)3.2 T-type Ca2+ channel-dependent activation of ERK in paraventricular thalamus modulates acid-induced chronic muscle pain. J Neurosci 30 10360 PMID: 20685979
Domin et al (2019) Characterization of the brain penetrant neuropeptide Y Y2 receptor antagonist SF-11. ACS Chem Neurosi 10 3454 PMID: 31267743
Kim et al (2018) Activation of miR-21-Regulated Pathways in Immune Aging Selects against Signatures Characteristic of Memory T Cells. Cell Rep 25 2148 PMID: 30463012
Li et al (2018) Upregulation of IRS1 Enhances IGF1 Response in Y537S and D538G ESR1 Mutant Breast Cancer Cells. Endocrinology 159 285 PMID: 29029116
Guo et al (2016) Selective Disruption of Metabotropic Glutamate Receptor 5-Homer Interactions Mimics Phenotypes of Fragile X Syndrome in Mice. J Neurosci 36 2131 PMID: 26888925
Tuvikene et al (2016) AP-1 Transcription Factors Mediate BDNF-Positive Feedback Loop in Cortical Neurons. J Neurosci 36 1290 PMID: 26818516
Sovadinova et al (2015) Phosphatidylcholine Specific PLC-Induced Dysregulation of Gap Junctions, a Robust Cellular Response to Environmental Toxicants, and Prevention by Resveratrol in a Rat Liver Cell Model. Oncogene 10 e0124454 PMID: 26023933
Zhao et al (2015) IL-13Rα2 mediates PNR-induced migration and metastasis in ERα-negative breast cancer. Nature 34 1596 PMID: 24747967
Do-Monte et al (2015) A temporal shift in the circuits mediating retrieval of fear memory. J Neuroinflammation 519 460 PMID: 25600268
Liu et al (2015) Hyperphosphate-Induced Myocardial Hypertrophy through the GATA-4/NFAT-3 Signaling Pathway Is Attenuated by ERK Inhibitor Treatment. Mol Cancer 5 79 PMID: 25999956
Koutsioumpa et al (2015) Receptor protein tyrosine phosphatase β/ζ is a functional binding partner for vascular endothelial growth factor. J Neurosci 14 19 PMID: 25644401
Briz et al (2015) Activity-dependent rapid local RhoA synthesis is required for hippocampal synaptic plasticity. Exp Hematol Oncol 35 2269 PMID: 25653381
Koerber et al (2015) Analysis of the anti-proliferative and the pro-apoptotic efficacy of Syk inhibition in multiple myeloma. Int J Cancer 4 21 PMID: 26251761
Choi et al (2015) SDF-1α stiffens myeloma bone marrow mesenchymal stromal cells through the activation of RhoA-ROCK-Myosin II. J Neurosci 136 E219 PMID: 25137150
Christianson et al (2014) Learned stressor resistance requires extracellular signal-regulated kinase in the prefrontal cortex. Front Behav Neurosci 8 348 PMID: 25324750
Morse et al (2013) Label-free integrative pharmacology on-target of opioid ligands at the opioid receptor family. BMC Pharmacol Toxicol 14 17 PMID: 23497702
Nemoto et al (2013) Angiotensin II produces nociceptive behavior through spinal AT1 receptor-mediated p38 mitogen-activated protein kinase activation in mice. Mol Pain 9 38 PMID: 23898828
Breshears et al (2012) A disintegrin and metalloproteinase 17 (ADAM17) and epidermal growth factor receptor (EGFR) signaling drive the epithelial response to Staphylococcus aureus toxic shock syndrome toxin-1 (TSST-1). J Biol Chem 287 32578 PMID: 22833676
Gangoiti et al (2012) Ceramide 1-phosphate stimulates proliferation of C2C12 myoblasts. Biochimie 94 597 PMID: 21945811
Schulz et al (2012) Phenotype-based high-content chemical library screening identifies STAT as inhibitors of in vivo lymphangiogenesis. Proc Natl Acad Sci U S A 109 E2665 PMID: 22949700
Arora et al (2012) Expression of protein-tyrosine phosphatases in Acute Myeloid Leukemia cells: FLT3 ITD sustains high levels of DUSP6 expression. Cell Commun Signal 10 19 PMID: 22784513
Hodges et al (2012) Signaling pathways used by EGF to stimulate conjunctival goblet cell secretion. Exp Eye Res 103 99 PMID: 22975404
Lee et al (2012) Fucoidan from seaweed Fucus vesiculosus inhibits migration and invasion of human lung cancer cell via PI3K-Akt-mTOR pathways. PLoS One 7 e50624 PMID: 23226337
Le et al (2010) The glutamate release inhibitor R.zole decreases migration, invasion, and proliferation of melanoma cells. J Invest Dermatol 130 2240 PMID: 20505744
Melemedjian et al (2010) IL-6- and NGF-induced rapid control of protein synthesis and nociceptive plasticity via convergent signaling to the eIF4F complex. J Neurosci 30 15113 PMID: 21068317
Beshir et al (2010) Raf kinase inhibitor protein suppresses nuclear factor-κB-dependent cancer cell invasion through negative regulation of matrix metalloproteinase expression. Cancer Lett 299 137 PMID: 20855151
Ishida et al (2010) Phosphorylation of Junb family proteins by the Jun N-terminal kinase supports tissue regeneration in zebrafish. Dev Biol 340 468 PMID: 20144602
He and Aizenman (2010) ERK signaling leads to mitochondrial dysfunction in extracellular zinc-induced neurotoxicity. J Neurochem 114 452 PMID: 20412391
Braun et al (2010) Uridine triphosphate (UTP) induces profibrotic responses in cardiac fibroblasts by activation of P2Y2 receptors. J Mol Cell Cardiol 49 362 PMID: 20471392
Chotiner et al (2010) Assessment of the role of MAP kinase in mediating activity-dependent transcriptional activation of the immediate early gene Arc/Arg3.1 in the dentate gyrus in vivo. Learn Mem 17 117 PMID: 20154358
Ito et al (2010) Synergistic growth inhibition of anaplastic large cell lymphoma cells by combining cellular ALK gene silencing and a low dose of the kinase inhibitor U0126. Cancer Gene Ther 17 633 PMID: 20448669
Noskovičová et al (2018) Cub domain-containing protein 1 negatively regulates TGF-β signaling and myofibroblast differentiation. Am J Physiol Lung Cell Mol Physiol 314 L695 PMID: 29351434
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Emery et al (2014) Separate cyclic AMP sensors for neuritogenesis, growth arrest, and survival of neuroendocrine cells. J Biol Chem 289 10126 PMID: 24567337
Heckler et al (2014) ERK/MAPK regulates ERRγ expression, transcriptional activity and receptor-mediated tamox. resistance in ER+ breast cancer. FEBS J 281 2431 PMID: 24684682
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Dohgu and Banks (2008) Lipopolysaccharide-enhanced transcellular transport of HIV-1 across the blood-brain barrier is mediated by the p38 mitogen-activated protein kinase pathway. Exp Neurol 210 740 PMID: 18295207
Lim et al (2008) The novel adipocytokine visfatin exerts direct cardioprotective effects. J Cell Mol Med 12 1395 PMID: 18400051
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Gallagher et al (2004) Extracellular signal-regulated protein kinase activation is required for metabotropic glutamate receptor-dependent long-term depression in hippocampal area CA1. J Neuroinflammation 24 4859 PMID: 15152046
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Experiment.
By
Chi Ngo on 09/28/2024
分析类型： In Vitro
种属： Human
细胞系/组织： Gastic epithelical cells (AGS)
To investigate if the induction of Snail1 by Helicobacter pylori infection in gastric epithelial cells AGS was regulated by the MEK/ERK pathway.
Aliquot the reconstituted compound to avoid freezing and thawing repeatedly.
Used to block MEK signaling..
By
MARINA KOUTSIOUMPA on 10/13/2022
分析类型： In Vitro
种属： Human
Pancreatic cancer cells were pretreated for 2 hours with U0126 followed by conventional chemotherapeutics. MEK inhibition had an additive effect on cancer cell’s viability upon 3 days of treatment.
Used for Migration assays.
By
Anonymous on 07/01/2020
分析类型： In Vitro
种属： Human
细胞系/组织： A549 or MDAMB231
All MAPK inhibitors (ZM336372: c-RAF inhibitor; UO126: MEK1/MEK2 inhibitor, SB203580: p38 inhibitor) were used at 10 μM
We ordered this product, combining with another inhibitor, to confirm the migration.To confirm that tested product induces migration, we also screen all MAPK inhibitors and MIF receptor antagonists
Effect of MEK inhibitor on E0771 extracellular flux.
By
Anonymous on 10/10/2018
分析类型： In Vitro
种属： Mouse
细胞系/组织： E0771
Extracellular flux analysis (Seahorse experiment) to examine the effect of MEK inhibitor in breast cancer cells. 5-10uM dose used.
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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 U0126
