ProductBackground:OncePI3-Kreactionarecomplete,thePIP3detectorproteinandthefluorescentprobeareadded.Polarization(mP)valuesdecreaseasprobe,bindingtothePIP3detector,isdisplacedbythePIP3producedbyenzymaticactivity.
ClassIPhosphoinositide3-kinases(PI3-K),areubiquitouslyexpressedlipidkinaseswhichphosphorylatePI(4,5)P2(PIP2)atthe3-hydroxyloftheinositolringproducingPIP3hasshowntobeanimportantlipidsecondmessengerwithkeyrolesinfundamentalcellularresponsessuchasproliferationandsurvival.DuetotheseinterestingBIOLOGicalroles,PI3-KandPIP3havebecomeattractivetargetsforresearchanddrugdevelopmentinmanydiseasesincludinginflammationandcancer.
FeaturedinPublications:
1.Drees,B.E.,A.Weipert,etal.(2003)."Competitivefluorescencepolarizationassaysforthedetectionofphosphoinositidekinaseandphosphataseactivity."CombChemHighThroughputScreen6(4):321-330.
2.Dehnhardt,C.M.,MansourTarekS.(2009)."LeadOptimizationofN-3-Substituted7-MorpholinotriazolopyrimidinesasDualPhosphoinositide3-Kinase/MammalianTargetofRapamycinInhibitors:DiscoveryofPKI-402."J.Med.Chem.
3.Safina,B.S.,S.Baker,etal.(2012)."DiscoveryofNovelPI3-KinasedSpecificInhibitorsfortheTreatmentofRheumatoidArthritis:TamingCYP3A4Time-DependentInhibition."JournalofMedicinalChemistry55(12):5887–5900.
4.Heffron,T.P.,R.A.Heald,etal.(2016)."TheRationalDesignofSelectiveBenzoxazepinInhibitorsoftheδ-IsoformofPhosphoinositide3-KinaseCulminatingintheIdentificationof(S)-2-((2-(1-isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide(GDC-0326)."JournalofMedicinalChemistry.DOI:10.1021/acs.jmedchem.5b01483
RelatedProducts:
ClassIPI3KActivityAssays:Echelonhasmultipleformatsavailable.PleaseseethePI3-KAssayComparisonChart formoreinformation.
ClassIIIPI3KActivityAssay(K-3000)
LipidMassELISA's:PIP3MassELISA(K-2500s)andPI(4,5)P2MassELISA(K-4500)
HumanPI3KEnzymes:alpha(p110α/p85α),beta(p110β/p85alphα),PI3KαααE545K–ActiveMutant(p110α/p85α)
MousePI3KEnzyme:PI3K(p110α/p85α)
PI3KInhibitors
OptimizedPI3Kenzymebuffer(K-KBZ)
NoticetoPurchaser:EchelonBiosciencesproductsaresoldforresearchanddevelopmentpurposesonlyandarenottobeincorporatedintoproductsforresalewithoutwrittenpermissionfromEchelonBiosciences.Thiskitandallnon-rADIoactive,competitiveassaysfordeterminingphosphoinositide-3-kinase(PI3-K)activityarecoveredbyEchelonBiosciencesInc.U.S.Patent7,067,269.Thepurchaseofthisproductincludesalimited,non-transferableimmunityfromsuitundertheforegoingpatentclaimsforusingonlythisamountofproductforthepurchaser'sowninternalresearch.
ProductKeywords:PI3-Kinase,PI3K,Phosphatidylinositol3-kinases,PI3-kinases,PI3Ks,K-1000
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