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- U0126 abstract "U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with IC50 of 72 nM for MEK1 and 58 nM for MEK2. U0126 inhibited anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both extracellular signal-regulated kinase (ERK) and mammalian target of rapamycin (mTOR)-p70(S6K) pathways. The effects of U0126 on the growth of eight human breast cancer cell lines shown that U0126 selectively repressed anchorage-independent growth of MDA-MB231 and HBC4 cells, two lines with constitutively activated ERK. Loss of contact with substratum triggers apoptosis in many normal cell types, a phenomenon termed anoikis. U0126 sensitized MDA-MB231 and HBC4 to anoikis, i.e., upon treatment with U0126, cells deprived of anchorage entered apoptosis.U0126 is also a weak inhibitor of PKC, Raf, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, Cdk2 and Cdk4.".
- U0126 casNumber "109511-58-2".
- U0126 iupacName "(2-aminophenylthio)butadiene".
- U0126 iupacName "1,4-diamino-2,3-dicyano-1,4-bis".
- U0126 thumbnail U0126.svg?width=300.
- U0126 wikiPageID "10066732".
- U0126 wikiPageLength "2683".
- U0126 wikiPageOutDegree "6".
- U0126 wikiPageRevisionID "682865599".
- U0126 wikiPageWikiLink Apoptosis.
- U0126 wikiPageWikiLink Category:Protein_kinase_inhibitors.
- U0126 wikiPageWikiLink Fibroblast.
- U0126 wikiPageWikiLink Fibroblasts.
- U0126 wikiPageWikiLink Kinase.
- U0126 wikiPageWikiLink MAP2K1.
- U0126 wikiPageWikiLink MAP2K2.
- U0126 wikiPageWikiLinkText "U0126".
- U0126 alt "Skeletal formulap".
- U0126 alt "Space-filling model".
- U0126 c "18".
- U0126 casNumber "109511".
- U0126 chembl "34704".
- U0126 h "16".
- U0126 hasPhotoCollection U0126.
- U0126 image "U0126-3D-spacefill.png".
- U0126 iupacName "14".
- U0126 iupacName "butadiene".
- U0126 molecularWeight "380.49".
- U0126 n "6".
- U0126 s "2".
- U0126 verifiedfields "changed".
- U0126 verifiedrevid "447749408".
- U0126 width "240".
- U0126 wikiPageUsesTemplate Template:Drugbox.
- U0126 wikiPageUsesTemplate Template:Enzyme-stub.
- U0126 wikiPageUsesTemplate Template:Multiple_issues.
- U0126 wikiPageUsesTemplate Template:Refbegin.
- U0126 wikiPageUsesTemplate Template:Refend.
- U0126 subject Category:Protein_kinase_inhibitors.
- U0126 type Article.
- U0126 type ChemicalSubstance.
- U0126 type Drug.
- U0126 type Article.
- U0126 type Chemical.
- U0126 type Inhibitor.
- U0126 type ChemicalObject.
- U0126 type Thing.
- U0126 type Q8386.
- U0126 comment "U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with IC50 of 72 nM for MEK1 and 58 nM for MEK2. U0126 inhibited anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both extracellular signal-regulated kinase (ERK) and mammalian target of rapamycin (mTOR)-p70(S6K) pathways.".
- U0126 label "U0126".
- U0126 sameAs U0126.
- U0126 sameAs U0126.
- U0126 sameAs m.02q0q1k.
- U0126 sameAs Q7863562.
- U0126 sameAs Q7863562.
- U0126 wasDerivedFrom U0126?oldid=682865599.
- U0126 depiction U0126.svg.
- U0126 isPrimaryTopicOf U0126.