PADI4-IN-1-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEPADI4-IN-1Cat.No.:HY-175518分子式: C₂₁H₂₃NO₃分子量: 337.41作用靶点: ProteinArginineDeiminase作用通路: Epigenetics储存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性PADI4-IN-1是一种强效的肽基精氨酸脱亚胺酶4(PADI4)抑制剂，其IC50值为1.5μM，选择性指数(SI)(PADI1/PADI4)为52.1。PADI4-IN-1能够抑制细胞瓜氨酸化事件。PADI4-IN-1可用于炎症相关研究，如类风湿性关节炎[1]。IC50&TargetPADI41.5μM(IC50)体外研究PADI4-IN-1(Compound7)(10-100μM,50mins)decreasestotalcellularcitrullinationeventsandhistoneH3citrullinationmediatedbyPADI4inHL-60celllysates[1].WesternBlotAnalysis[1]CellLine:HL-60cellsConcentration:10and100μMIncubationTime:50minsResult:DecreasedtotalHL-60cellularcitrullinationeventsandhistoneH3citrullinationmediatedbyPADI4.体内研究PADI4-IN-1(Compound7)(20mg/kg,i.p.,atdays3,4,5,6,and7)amelioratestheseverityandpathologicprogressincollagentypeIIantibody/LPS(HY-D1056)inducedrheumatoidarthritismicemodels[1].AnimalModel:CollagentypeIIantibody/LPS(HY-D1056)inducedrheumatoidarthritismicemodels[1]1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEDosage:20mg/kgAdministration:IntraperitoneallyinjectionResult:Decreasedthearthritisscoreofthemiceby66%treatedatdays4,5,6,and7.Decreasedthearthritisscoreofthemiceby100%treatedatdays3and4.ReducedtheexpressionofIL-6,IL-1β,IFN-γ,RANKL,IL-17A,CXCL15,ANXA2,HIF-1α,iNOS,andTNF-αtreatedatdays3and4.Reducedinflammatorycellinflux,pannusformation,cartilagedestruction,cartilageremnant,edema,andaccumulationofinflammatorycells(mononuclearcellsandneutrophil).Reducedtheerosionofcartilageandbone.Reducedthelevelsofcitrullinatedantigens.REFERENCESYangCW,etal.Synthesisandevaluationofanovelclassofspiro[chromene-2,2'-indoline]derivativesaspotentinhibitorsofpeptidylargininedeiminaseIVtotreatrheumatoidarthritis.EurJMedChem.2025Nov15;298:117985.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel