U-0126, MEK inhibitor
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Catalog numberSIH-380-5MG
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PricePlease ask
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Size5 mg
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Stock availabilitIn StockIn Stock
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CAS number109511-58-2
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DescriptionMEK inhibitor
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Molecular weight380,5 g/mol
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Primary research fieldsCell Signaling
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Other name1,4-Diamino-2,3-dicyano-1,4-bis[2-aminophenylthio]butadiene
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Product categorySmall Molecules
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Product typeInhibitor
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Chemical formulaC18H16N6S2
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OriginSynthetic
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Purity pourcentage>98%
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Soluble inSoluble in DMSO (>10 mg/ml), 100% ethanol (2 mg/ml)
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Physical appearanceWhite solid
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Storage recommendations-20ºC
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Shipping recommendationsShipped Ambient
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Safety informationClassification: Caution: Substance not yet fully tested. Safety Phrases: S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection
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PubChem number3006531
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Scientific contextU-0126 is a novel, potent and selective MEK inhibitor (MEK1; IC50=72nM, MEK2; IC50=58nM). Inhibits AP-1 transcription activity. Blocks the production of inflammatory cytokines and matrix metalloproteinases. Binding of extracellular growth factors to cell surface receptors often results in activation of the mitogen-activated protein kinase (MAPK). MAPK is regulated by MAPK kinase, also called MEK. Deprivation of growth factors during cell culture or intracellular MEK inhibition leads to inhibition of proliferation and apoptotic cell death. N Blank et al. (2002) have shown that U0126, a common used MEK inhibitor and compound that itself has no intrinsic fluorescence in vitro but develops an intensive fluorescence during cell culture which can be observed in all fluorescence channels with predominance in the FL1 channel (525nm).
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Bibliography1. Duncia J.V., et a.l (1998) Bioorg. Med. Chem. Lett. 8(20): 2839-44. 2. Favata M.F., et al. (1998) J. Biol. Chem. 273(29): 18623-32. 3. Davies S.P., et al. (2000) Biochem. J. 351(Pt1): 95-105. 4. Namura S., et al. (2001) Proc. Natl. Acad. Sci. U.S.A. 98(20): 11569-74.
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Release date17-Jul-2013
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PubMed numberRefer to PubMed
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Tested applicationsTo be tested
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Tested reactivityTo be tested
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Representative figure legendChemical structure of U-0126 (SIH-380), a MEK inhibitor. CAS #: 109511-58-2. Molecular Formula: C18H16N6S2. Molecular Weight: 380.5 g/mol. Chemical structure of U-0126, a MEK inhibitor (SIH-380). CAS # 109511-58-2. Molecular Formula: C18H16N6S2.
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Warning informationNon-hazardous
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Country of productionCanada
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Total weight kg0.25
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Net weight g0.005
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Additional descriptionTissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.
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Gene target
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Gene symbolHLA-U, UTS2, CENPU
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Short nameU-0126, MEK inhibitor
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Alternative nameU-0126, MEK suppressor
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Gene info
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Identity
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Gene
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Long gene namemajor histocompatibility complex, class I, U (pseudogene)
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Synonyms gene
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Synonyms gene name
- HLA-21 pseudogene
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Synonyms
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GenBank acession
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Locus
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Discovery year2004-01-16
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Entrez gene record
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RefSeq identity
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Classification
- Histocompatibility complex
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VEGA ID
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Locus Specific Databases
Gene info
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Identity
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Gene
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Long gene nameurotensin 2
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Synonyms
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Synonyms name
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GenBank acession
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Locus
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Discovery year2000-03-22
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Entrez gene record
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Pubmed identfication
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RefSeq identity
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Classification
- Receptor ligands
- Neuropeptides
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VEGA ID
Gene info
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Identity
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Gene
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Long gene namecentromere protein U
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Synonyms gene
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Synonyms gene name
- MLF1 interacting protein
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Synonyms
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Synonyms name
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GenBank acession
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Locus
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Discovery year2003-07-17
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Entrez gene record
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Pubmed identfication
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RefSeq identity
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Classification
- Constitutive centromere associated network
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VEGA ID