U0126

Pricing Availability Delivery Time Qty
Cat.No. 1144 - U0126 | C18H16N6S2 | CAS No. 109511-58-2
Description: Potent, selective inhibitor of MEK1 and 2
Chemical Name: 1,4-Diamino-2,3-dicyano-1,4-bis[2-aminophenylthio]butadiene
Datasheet
Citations (76)
Literature
Pathways

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. Also available as part of the MAPK Cascade Inhibitor Tocriset™ and MAPK Inhibitor Tocriset™. Negative control U0124 (Cat. No. 1868) also available.

Compound Libraries

U0126 is also offered as part of the Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 380.48
Formula C18H16N6S2
Storage 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

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 38.05 100

Preparing Stock Solutions

The following data is based on the product molecular weight 380.48. 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 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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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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.

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Keywords: U0126, supplier, Potent, selective, inhibitors, inhibits, MEK1, MEK2, Mitogen-Activated, Protein, Kinase, Kinases, MEK, Stem, Cell, Proliferation, MEK, Tocris Bioscience

76 Citations for U0126

Citations are publications that use Tocris products. Selected citations for U0126 include:

Liang et al (2014) δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes. J Neuroinflammation 171 5417 PMID: 25052197

Alpár et al (2014) Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling. Cell Rep 5 4421 PMID: 25030704

Wan et al (2014) Retinal injury, growth factors, and cytokines converge on β-catenin and pStat3 signaling to stimulate retina regeneration. Neuroscience 9 285 PMID: 25263555

Voon et al (2013) EMT-induced stemness and tumorigenicity are fueled by the EGFR/Ras pathway. PLoS One 8 e70427 PMID: 23950932

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) 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

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

Jensen et al (2013) An ERK-p38 subnetwork coordinates host cell apoptosis and necrosis during coxsackievirus B3 infection. J Neurosci 13 67 PMID: 23332156

Meyer et al (2013) Distinct dedifferentiation processes affect caveolin-1 expression in hepatocytes. J Pharmacol Exp Ther 11 6 PMID: 23339737

Philips et al (2013) MAPK establishes a molecular context that defines effective training patterns for long-term memory formation. J Neurosci 33 7565 PMID: 23616561

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 statins 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

Ito et al (2011) Interleukin-2 Functions in Anaplastic Large Cell Lymphoma Cells through Augmentation of Extracellular Signal-Regulated Kinases 1/2 Activation. Int J Biomed Sci 7 181 PMID: 23675235

Sbroggiò et al (2011) ERK1/2 activation in heart is controlled by melusin, focal adhesion kinase and the scaffold protein IQGAP1. J Cell Sci 124 3515 PMID: 22010199

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

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

Rubert et al (2011) Bim and Mcl-1 exert key roles in regulating JAK2V617F cell survival. BMC Cancer 11 24 PMID: 21247487

Hsu et al (2011) 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. Cell Commun Signal 18 61 PMID: 21859479

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

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

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

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

Le et al (2010) The glutamate release inhibitor Riluzole 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

Pera et al (2010) Cigarette smoke and lipopolysaccharide induce a proliferative airway smooth muscle phenotype. J Neurosci 11 48 PMID: 20429916

Kolber et al (2010) Activation of metabotropic glutamate receptor 5 in the amygdala modulates pain-like behavior. Nat Commun 30 8203 PMID: 20554871

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

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

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

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

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

Khan et al (2007) Catecholaminergic control of mitogen-activated protein kinase signaling in paraventricular neuroendocrine neurons in vivo and in vitro: a proposed role during glycemic challenges. Nat Commun 27 7344 PMID: 17611287

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

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 Neurosci 5 40 PMID: 17018141

O'Riordan et al (2006) Regulation of nuclear factor κB in the hippocampus by group I metabotropic glutamate receptors. Cell Host Microbe 26 4870 PMID: 16672661

Pierre et al (2004) PAM mediates sustained inhibition of cAMP signaling by sphingosine-1-phosphate. EMBO J 23 3031 PMID: 15257286

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

Dominguez et al (2004) Morphological effects of estrogen on cholinergic neurons in vitro involves activation of extracellular signal-regulated kinases. J Neurosci 24 982 PMID: 14749443

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

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

Yang et al (2016) The PDGF-BB-SOX7 axis-modulated IL-33 in pericytes and stromal cells promotes metastasis through tumour-associated macrophages. Nat Commun 7 11385 PMID: 27150562

Lee et al (2016) Mincle-mediated translational regulation is required for strong nitric oxide production and inflammation resolution. Cardiorenal Med 7 11322 PMID: 27089465

Dang et al (2016) 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. Korean J Physiol Pharmacol 13 12 PMID: 26780950

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

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

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

Schubert et al (2014) Paraneoplastic CDR2 and CDR2L antibodies affect Purkinje cell calcium homeostasis. Acta Neuropathol 128 835 PMID: 25341622

Babu et al (2014) TGFβ-mediated suppression of CD248 in non-cancer cells via canonical Smad-dependent signaling pathways is uncoupled in cancer cells. BMC Cancer 14 113 PMID: 24555435

Wan et al (2014) Cathelicidin LL-37 induces time-resolved release of LTB4 and TXA2 by human macrophages and triggers eicosanoid generation in vivo. FASEB J 28 3456 PMID: 24736410


Do you know of a great paper that uses U0126 from Tocris? If so please let us know.

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MAPK

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