LY2090314-GMP-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELY2090314(GMP)Cat.No.:HY-16294GCASNo.:603288-22-8分⼦式:C₂₈H₂₅FN₆O₃分⼦量:512.53作⽤靶点:GSK-3作⽤通路:PI3K/Akt/mTOR;StemCell/Wnt储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性LY2090314(GMP)GMP级别的LY2090314(HY-16294)。GMP级别的⼩分⼦可⽤做细胞疗法中的辅助试剂。LY2090314⼀种有效的GSK-3抑制剂，抑制GSK-3α和GSK-3β，IC50值分别为1.5nM和0.9nM。体外研究LY2090314(GMP)(20nM)promotesatime-dependentstabilizationofβ-catenintotalproteinaswellasaninductionofAxin2.LY2090314(GMP)ishighlyselectivetowardsGSK3asdemonstratedbyitsfoldselectivityrelativetoalargepanelofkinases.LY2090314(GMP)potentlyinducesapoptoticcelldeathinapanelofmelanomacelllinesirrespectiveofBRAFmutationstatus.Celldeathinducedby(GMP)isdependentonβ-cateninandGSK3βknockdownincreasesthesensitivityofcellsto(GMP).(GMP)remainsactiveincelllinesresistanttoPLX4032andhasanindependentmechanismofaction[2].体内研究LY2090314(GMP)exhibitshighclearance(approximatinghepaticbloodflow)andamoderatevolumeofdistribution(appr1-2L/kg)resultinginrapidelimination(half-lifeappr0.4,0.7,and1.8-3.4hoursinrats,dogs,andhumans,respectively).LY2090314(GMP)israpidlyclearedbyextensivemetabolismwithnegligiblecirculatingmetaboliteexposuresduetobiliaryexcretionofmetabolitesintofeceswithnoapparentintestinalreabsorption[1].LY2090314(GMP)(25mg/kgQ3D,i.v.)elevatesAxin2geneexpressioninvivo,demonstratessingleagentactivityintheA375xenograftmodelofmelanomaandenhancestheefficacyofDTIC[2].户使⽤本产品发表的科研⽂献•Nature.2025Jun;642(8067):508-518.•CellRes.2025Aug29.1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•CellRes.2022Jun;32(6):513-529.•NatCommun.2019Sep25;10(1):4364.•CellRep.2025Sep29;44(10):116361.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].AtkinsonJM,etal.ActivatingtheWnt/β-CateninPathwayfortheTreatmentofMelanoma--ApplicationofLY2090314,aNovelSelectiveInhibitorofGlycogenSynthaseKinase-3.PLoSOne.2015Apr27;10(4):e0125028.[2].Zamek-GliszczynskiMJ,etal.Pharmacokinetics,metabolism,andexcretionoftheglycogensynthasekinase-3inhibitorLY2090314inrats,dogs,andhumans:acasestudyinrapidclearancebyextensivemetabolismwithlowcirculatingmetaboliteexposure.DrMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For