BBC0403-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBBC0403Cat.No.:HY-162514CASNo.:2644662-83-7分⼦式:C₂₁H₂₂N₂O₅分⼦量:382.41作⽤靶点:EpigeneticReaderDomain作⽤通路:Epigenetics储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性BBC0403⼀种选择性BRD2抑制剂，对BRD2(BD2)和BRD2(BD1)的Kd分别为7.64μM和41.37μM。BBC0403对BRD2的选择性⾼于BRD3和BRD4。BBC0403具有⾻关节炎(OA)研究的潜⼒。IC50&TargetBRD2(BD2)BRD2(BD1)7.64μM(Kd)41.37μM(Kd)体外研究BBC0403(5ꢀμM,10ꢀμMand20ꢀμM,12ꢀh)reducestheexpressionofcatabolicfactors,prostaglandinE2(PGE2)productionandextracellularmatrix(ECM)degradation.BBC0403preventsOAbyinhibitingNF-κBandMAPKsignalling[1].体内研究BBC0403(5-10μg/kg;i.a.;onceperweek;6weeks)preventsOAcartilagedegradationinmice[1].AnimalModel:MaleC57BL/6mice(12ꢀweeksold;18-20ꢀg)bearingosteoarthritis(OA)[1]Dosage:5μg/kg,10μg/kgAdministration:Intra-articular(i.a.)injection;onceperweek;6weeksResult:PreventedOAcartilagedegradationinmice.REFERENCES[1].HyemiLee,etal.BRD2-specificinhibitor,BBC0403,inhibitstheprogressionofosteoarthritispathogenesisinosteoarthritis-induced1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEC57BL/6malemice.BrJPharmacol.2024Apr10.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792ax:02