Catalog Number: 1144
Chemical Name: 1,4-Diamino-2,3-dicyano-1,4-bis[2-aminophenylthio]butadiene
Biological Activity
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.

Available as part of the MAPK Cascade Inhibitor Tocriset™ and MAPK Inhibitor Tocriset™. Negative Control also available.

Technical Data
  • M.Wt:
    380.48
  • Formula:
    C18H16N6S2
  • Solubility:
    Soluble to 100 mM in DMSO
  • Storage:
    Desiccate at +4°C
  • CAS No:
    109511-58-2
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.
Additional Information
Other Product-Specific Information:
Background References
  1. Specificity and mechanism of action of some commonly used protein kinase inhibitors.
    Davies et al.
    Biochem.J., 2000;351:95
  2. MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.
    Duncia et al.
    Bioorg.Med.Chem.Lett., 1998;8:2839
  3. Identification of a novel inhibitor of mitogen-activated protein kinase kinase.
    Favata et al.
    J.Biol.Chem., 1998;273:18623
  4. Intravenous administraton of MEK inhibitor U0126 affords brain protection against forebrain ischemia and focal cerebral ischemia.
    Namura et al.
    Proc.Natl.Acad.Sci.U.S.A., 2001;98:11569
  5. Protein kinase C regulates human pluripotent stem cell self-renewal.
    Kinehara et al.
    PLoS One, 2013;8:e54122
Citations:

The citations listed below are publications that use Tocris products. Selected citations for U0126 include:

76 Citations: Showing 1 - 10
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  1. TRIB3 downregulation enhances doxorubicin-induced cytotoxicity in gastric cancer cells.
    Authors: Wu
    Arch Biochem Biophys 2017;622:26
  2. Opposing Actions of Fgf8a on Notch Signaling Distinguish Two Muller Glial Cell Populations that Contribute to Retina Growth and Regeneration.
    Authors: Wan and Goldman
    Cell?Rep 2017;19(4):849
  3. The PDGF-BB-SOX7 axis-modulated IL-33 in pericytes and stromal cells promotes metastasis through tumour-associated macrophages.
    Authors: Yang Et al.
    Nat Commun 2016;7:11385
  4. Mincle-mediated translational regulation is required for strong nitric oxide production and inflammation resolution.
    Authors: Lee Et al.
    Cardiorenal Med 2016;7:11322
  5. Bromodomain containing protein represses the Ras/Raf/MEK/ERK pathway to attenuate human hepatoma cell proliferation during HCV infection.
    Authors: Zhang Et al.
    Cancer Lett. 2016;371:107
  6. Apocynin prevents mitochondrial burdens, microglial activation, and pro-apoptosis induced by a toxic dose of methamphetamine in the striatum of mice via inhibition of p47phox activation by ERK.
    Authors: Dang Et al.
    Korean J Physiol Pharmacol 2016;13:12
  7. Hyperphosphate-Induced Myocardial Hypertrophy through the GATA-4/NFAT-3 Signaling Pathway Is Attenuated by ERK Inhibitor Treatment.
    Authors: Liu Et al.
    Mol Cancer 2015;5:79
  8. A temporal shift in the circuits mediating retrieval of fear memory.
    Authors: Do-Monte Et al.
    J Neuroinflammation 2015;519:460
  9. Analysis of the anti-proliferative and the pro-apoptotic efficacy of Syk inhibition in multiple myeloma.
    Authors: Koerber Et al.
    Int J Cancer 2015;4:21
  10. MAPK signaling downstream to TLR4 contributes to paclitaxel-induced peripheral neuropathy.
    Authors: Li Et al.
    Brain Behav.Immun. 2015;49:255
  11. Activity-dependent rapid local RhoA synthesis is required for hippocampal synaptic plasticity.
    Authors: Briz Et al.
    Exp Hematol Oncol 2015;35:2269
  12. IL-13Rα2 mediates PNR-induced migration and metastasis in ERα-negative breast cancer.
    Authors: Zhao Et al.
    Nature 2015;34:1596
  13. P2X7 Receptor Regulates Internalization of Antimicrobial Peptide LL-37 by Human Macrophages That Promotes Intracellular Pathogen Clearance.
    Authors: Tang Et al.
    J Immunol 2015;195:1191
  14. Macrophage migration inhibitory factor-CXCR4 is the dominant chemotactic axis in human mesenchymal stem cell recruitment to tumors.
    Authors: Lourenco Et al.
    J Immunol 2015;194:3463
  15. Receptor protein tyrosine phosphatase β/ζ is a functional binding partner for vascular endothelial growth factor.
    Authors: Koutsioumpa Et al.
    J Neurosci 2015;14:19
  16. SDF-1α stiffens myeloma bone marrow mesenchymal stromal cells through the activation of RhoA-ROCK-Myosin II.
    Authors: Choi Et al.
    J Neurosci 2015;136:E219
  17. 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.
    Authors: Sovadinova Et al.
    Oncogene 2015;10:e0124454
  18. Retinal injury, growth factors, and cytokines converge on β-catenin and pStat3 signaling to stimulate retina regeneration.
    Authors: Wan Et al.
    Neuroscience 2014;9:285
  19. Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling.
    Authors: Alpár Et al.
    Cell Rep 2014;5:4421
  20. Cathelicidin LL-37 induces time-resolved release of LTB4 and TXA2 by human macrophages and triggers eicosanoid generation in vivo.
    Authors: Wan Et al.
    FASEB J 2014;28:3456
  21. δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes.
    Authors: Liang Et al.
    J Neuroinflammation 2014;171:5417
  22. TGFβ-mediated suppression of CD248 in non-cancer cells via canonical Smad-dependent signaling pathways is uncoupled in cancer cells.
    Authors: Babu Et al.
    BMC Cancer 2014;14:113
  23. Paraneoplastic CDR2 and CDR2L antibodies affect Purkinje cell calcium homeostasis.
    Authors: Schubert Et al.
    Acta Neuropathol 2014;128:835
  24. EMT-induced stemness and tumorigenicity are fueled by the EGFR/Ras pathway.
    Authors: Voon Et al.
    PLoS One 2013;8:e70427
  25. Polycyclic aromatic hydrocarbon-induced signaling events relevant to inflammation and tumorigenesis in lung cells are dependent on molecular structure.
    Authors: Osgood Et al.
    PLoS One 2013;8:e65150
  26. The prolyl isomerase Pin1 acts synergistically with CDK2 to regulate the basal activity of estrogen receptor α in breast cancer.
    Authors: Lucchetti Et al.
    PLoS One 2013;8:e55355
  27. Effect of VIP on intracellular [Ca2+], extracellular regulated kinase 1/2, and secretion in cultured rat conjunctival goblet cells.
    Authors: Li Et al.
    Invest Ophthalmol Vis Sci 2013;54:2872
  28. MAPK establishes a molecular context that defines effective training patterns for long-term memory formation.
    Authors: Philips Et al.
    J Neurosci 2013;33:7565
  29. Acute mitochondrial inhibition by mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK) 1/2 inhibitors regulates proliferation.
    Authors: Ripple Et al.
    J Biol Chem 2013;288:2933
  30. Arc in the nucleus regulates PML-dependent GluA1 transcription and homeostatic plasticity.
    Authors: Korb Et al.
    Nat Neurosci 2013;16:874
  31. mTORC1 inhibition induces pain via IRS-1-dependent feedback activation of ERK.
    Authors: Melemedjian Et al.
    Pain 2013;154:1080
  32. An ERK-p38 subnetwork coordinates host cell apoptosis and necrosis during coxsackievirus B3 infection.
    Authors: Jensen Et al.
    J Neurosci 2013;13:67
  33. Distinct dedifferentiation processes affect caveolin-1 expression in hepatocytes.
    Authors: Meyer Et al.
    J Pharmacol Exp Ther 2013;11:6
  34. 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;
  35. Ceramide 1-phosphate stimulates proliferation of C2C12 myoblasts.
    Authors: Gangoiti Et al.
    Biochimie 2012;94:597
  36. Fucoidan from seaweed Fucus vesiculosus inhibits migration and invasion of human lung cancer cell via PI3K-Akt-mTOR pathways.
    Authors: Lee Et al.
    PLoS One 2012;7:e50624
  37. 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).
    Authors: Breshears Et al.
    J Biol Chem 2012;287:32578
  38. Expression of protein-tyrosine phosphatases in Acute Myeloid Leukemia cells: FLT3 ITD sustains high levels of DUSP6 expression.
    Authors: Arora Et al.
    Cell Commun Signal 2012;10:19
  39. Phenotype-based high-content chemical library screening identifies statins as inhibitors of in vivo lymphangiogenesis.
    Authors: Schulz Et al.
    Proc Natl Acad Sci U S A 2012;109:E2665
  40. Signaling pathways used by EGF to stimulate conjunctival goblet cell secretion.
    Authors: Hodges Et al.
    Exp Eye Res 2012;103:99
  41. Lipopolysaccharide-enhanced transcellular transport of HIV-1 across the blood-brain barrier is mediated by luminal microvessel IL-6 and GM-CSF.
    Authors: Dohgu Et al.
    Br J Pharmacol 2011;8:167
  42. Brain microvascular pericytes are immunoactive in culture: cytokine, chemokine, nitric oxide, and LRP-1 expression in response to lipopolysaccharide.
    Authors: Kovac Et al.
    J Neurosci 2011;8:139
  43. Targeting adenosine monophosphate-activated protein kinase (AMPK) in preclinical models reveals a potential mechanism for the treatment of neuropathic pain.
    Authors: Melemedjian Et al.
    Mol Pain 2011;7:70
  44. Interleukin-2 Functions in Anaplastic Large Cell Lymphoma Cells through Augmentation of Extracellular Signal-Regulated Kinases 1/2 Activation.
    Authors: Ito Et al.
    Int J Biomed Sci 2011;7:181
  45. JNK suppression is essential for 17β-Estradiol inhibits prostaglandin E2-Induced uPA and MMP-9 expressions and cell migration in human LoVo colon cancer cells.
    Authors: Hsu Et al.
    Cell Commun Signal 2011;18:61
  46. Rapid brain-derived neurotrophic factor-dependent sequestration of amygdala and hippocampal GABA(A) receptors via different tyrosine receptor kinase B-mediated phosphorylation pathways.
    Authors: Mou Et al.
    Respir Res 2011;176:72
  47. Thrombin-induced Migration and Matrix Metalloproteinase-9 Expression Are Regulated by MAPK and PI3K Pathways in C6 Glioma Cells.
    Authors: Kim Et al.
    Mol Cancer 2011;15:211
  48. ERK1/2 activation in heart is controlled by melusin, focal adhesion kinase and the scaffold protein IQGAP1.
    Authors: Sbroggiò Et al.
    J Cell Sci 2011;124:3515
  49. Bim and Mcl-1 exert key roles in regulating JAK2V617F cell survival.
    Authors: Rubert Et al.
    BMC Cancer 2011;11:24
  50. β1-Adrenergic receptors activate two distinct signaling pathways in striatal neurons.
    Authors: Meitzen Et al.
    J Neurochem 2011;116:984
  51. Uridine triphosphate (UTP) induces profibrotic responses in cardiac fibroblasts by activation of P2Y2 receptors.
    Authors: Braun Et al.
    J Mol Cell Cardiol 2010;49:362
  52. Phosphorylation of Junb family proteins by the Jun N-terminal kinase supports tissue regeneration in zebrafish.
    Authors: Ishida Et al.
    Dev Biol 2010;340:468
  53. Activation of metabotropic glutamate receptor 5 in the amygdala modulates pain-like behavior.
    Authors: Kolber Et al.
    Nat Commun 2010;30:8203
  54. IL-6- and NGF-induced rapid control of protein synthesis and nociceptive plasticity via convergent signaling to the eIF4F complex.
    Authors: Melemedjian Et al.
    J Neurosci 2010;30:15113
  55. Raf kinase inhibitor protein suppresses nuclear factor-κB-dependent cancer cell invasion through negative regulation of matrix metalloproteinase expression.
    Authors: Beshir Et al.
    Cancer Lett 2010;299:137
  56. Synergistic growth inhibition of anaplastic large cell lymphoma cells by combining cellular ALK gene silencing and a low dose of the kinase inhibitor U0126.
    Authors: Ito Et al.
    Cancer Gene Ther 2010;17:633
  57. 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.
    Authors: Chotiner Et al.
    Learn Mem 2010;17:117
  58. The glutamate release inhibitor Riluzole decreases migration, invasion, and proliferation of melanoma cells.
    Authors: Le Et al.
    J Invest Dermatol 2010;130:2240
  59. Cigarette smoke and lipopolysaccharide induce a proliferative airway smooth muscle phenotype.
    Authors: Pera Et al.
    J Neurosci 2010;11:48
  60. ERK signaling leads to mitochondrial dysfunction in extracellular zinc-induced neurotoxicity.
    Authors: He and Aizenman
    J Neurochem 2010;114:452
  61. 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
  62. BC1 regulation of metabotropic glutamate receptor-mediated neuronal excitability.
    Authors: Zhong Et al.
    J Neurosci 2009;29:9977
  63. The serum response factor and a putative novel transcription factor regulate expression of the immediate-early gene Arc/Arg3.1 in neurons.
    Authors: Pintchovski Et al.
    J Neurosci 2009;29:1525
  64. Proteomic analysis uncovers novel actions of the neurosecretory protein VGF in nociceptive processing.
    Authors: Riedl Et al.
    PLoS One 2009;29:13377
  65. Mechanisms underlying fibronectin-induced up-regulation of P2X4R expression in microglia: distinct roles of PI3K-Akt and MEK-ERK signalling pathways.
    Authors: Tsuda Et al.
    J Cell Mol Med 2009;13:3251
  66. 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.
    Authors: Magliaro and Saldanha
    Brain Res 2009;1283:14
  67. PKA and Epac cooperate to augment bradykinin-induced interleukin-8 release from human airway smooth muscle cells.
    Authors: Roscioni Et al.
    Respir Res 2009;10:88
  68. Lipopolysaccharide-enhanced transcellular transport of HIV-1 across the blood-brain barrier is mediated by the p38 mitogen-activated protein kinase pathway.
    Authors: Dohgu and Banks
    Exp Neurol 2008;210:740
  69. Catecholaminergic control of mitogen-activated protein kinase signaling in paraventricular neuroendocrine neurons in vivo and in vitro: a proposed role during glycemic challenges.
    Authors: Khan Et al.
    Nat Commun 2007;27:7344
  70. Insulin induces airway smooth muscle contraction.
    Authors: Schaafsma Et al.
    J Biomed Sci 2007;150:136
  71. 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 Neurosci 2006;5:40
  72. Regulation of nuclear factor κB in the hippocampus by group I metabotropic glutamate receptors.
    Authors: O'Riordan Et al.
    Cell Host Microbe 2006;26:4870
  73. 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
  74. Morphological effects of estrogen on cholinergic neurons in vitro involves activation of extracellular signal-regulated kinases.
    Authors: Dominguez Et al.
    J Neurosci 2004;24:982
  75. Extracellular signal-regulated protein kinase activation is required for metabotropic glutamate receptor-dependent long-term depression in hippocampal area CA1.
    Authors: Gallagher Et al.
    J Neuroinflammation 2004;24:4859
  76. PAM mediates sustained inhibition of cAMP signaling by sphingosine-1-phosphate.
    Authors: Pierre Et al.
    EMBO J 2004;23:3031
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