MedKooCat#:406432
Name:PF-4708671
CAS#:1255517-76-0
ChemicalFormula:C19H21F3N6
ExactMass:390.17798
MolecularWeight:390.40545
ElementalAnalysis:C,58.45;H,5.42;F,14.60;N,21.53
Synonym:PF4708671;PF-4708671;PF4708671.
IUPAC/ChemicalName:2-((4-(5-ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-5-(trifluoromethyl)-1H-benzo[d]imidazole
SMILESCode:FC(C1=CC=C2NC(CN3CCN(C4=NC=NC=C4CC)CC3)=NC2=C1)(F)F
S6K1(p70ribosomalS6kinase1)isactivatedbyinsulinandgrowthfactorsviathePI3K(phosphoinositide3-kinase)andmTOR(mammaliantargetofrapamycin)signallingpathways.S6K1regulatesnumerousprocesses,suchasproteinsynthesis,growth,proliferationandlongevity,anditsinhibitionhasbeenproposedasastrategyforthetreatmentofcancerandinsulinresistance.
1:LeontievaOV,DemidenkoZN,BlagosklonnyMV.S6Kingeroconversion.CellCycle.2013Oct15;12(20):3249-52.doi:10.4161/cc.26248.Epub2013Sep9.PubMedPMID:24036549.
2:AllardEK,GrujicM,FisoneG,KristenssonK.Prionformationcorrelateswithactivationoftranslation-regulatingprotein4E-BPandneuronaltranscriptionfactorElk1.NeurobiolDis.2013Oct;58:116-22.doi:10.1016/j.nBD.2013.05.014.Epub2013Jun3.PubMedPMID:23742760.
3:ParkerWE,OrlovaKA,ParkerWH,BirnbaumJF,KrymskayaVP,GoncharovDA,BaybisM,HelfferichJ,OkochiK,StraussKA,CrinoPB.RapamycinpreventsseizuresafterdepletionofSTRADAinarareneurodevelopmentaldisorder.SciTranslMed.2013Apr24;5(182):182ra53.doi:10.1126/scitranslmed.3005271.PubMedPMID:23616120;PubMedCentralPMCID:PMC3720125.
4:RajanMR,FagerholmS,JönssonC,KjølhedeP,TurkinaMV,StrålforsP.PhosphorylationofIRS1atserine307inresponsetoinsulininhumanADIpocytesisnotlikelytobecatalyzedbyp70ribosomalS6kinase.PLoSOne.2013;8(4):e59725.doi:10.1371/journal.pone.0059725.Epub2013Apr2.PubMedPMID:23565163;PubMedCentralPMCID:PMC3614923.
5:ChoiHN,JinHO,KimJH,HongSE,KimHA,KimEK,LeeJK,ParkIC,NohWC.InhibitionofS6K1enhancesglucosedeprivation-inducedcelldeathviadownregulationofanti-apoptoticproteinsinMCF-7breastcancercells.BiochemBiophysResCommun.2013Mar1;432(1):123-8.doi:10.1016/j.bbrc.2013.01.074.Epub2013Jan29.PubMedPMID:23376066.
6:DiR,WuX,ChangZ,ZhaoX,FengQ,LuS,LuanQ,HemmingsBA,LiX,YangZ.S6KinhibitionrenderscardiacprotectionagainstmyocardialinfarctionthroughPDK1phosphorylationofAkt.BiochemJ.2012Jan1;441(1):199-207.doi:10.1042/BJ20110033.PubMedPMID:21906027.
7:RosnerM,SchipanyK,HengstschlägerM.p70S6K1nuclearlocalizationdependsonitsmTOR-mediatedphosphorylationatT389,butnotonitskinaseactivitytowardsS6.AminoAcids.2012Jun;42(6):2251-6.doi:10.1007/s00726-011-0965-4.Epub2011Jun28.PubMedPMID:21710263.
8:BilangesB,VanhaesebroeckB.Anewtooltodissectthefunctionofp70S6kinase.BiochemJ.2010Oct15;431(2):e1-3.doi:10.1042/BJ20101445.PubMedPMID:20874709.
9:PearceLR,AltonGR,RichterDT,KathJC,LingardoL,ChapmanJ,HwangC,AlessiDR.CharacterizationofPF-4708671,anovelandhighlyspecificinhibitorofp70ribosomalS6kinase(S6K1).BiochemJ.2010Oct15;431(2):245-55.doi:10.1042/BJ20101024.PubMedPMID:20704563.
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