Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEADAR1-IN-1Cat.No.:HY-175243CASNo.:2734853-87-1分子式:C??H??F?N?O?S分子量:493.39作用靶點(diǎn):AdenosineDeaminase;Apoptosis作用通路:MetabolicEnzyme/Protease;Apoptosis儲(chǔ)存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性ADAR1-IN-1是一種強(qiáng)效的ADAR1抑制劑。ADAR1-IN-1顯著抑制了DU-145細(xì)胞的增殖(IC50=1.11μM)、克隆形成、遷移和侵襲，并誘導(dǎo)細(xì)胞周期阻滯和凋亡(apoptosis)。ADAR1-IN-1能安全有效地抑制腫瘤生長(zhǎng)。ADAR1-IN-1可用于前列腺癌(PCa)的研究[1]。[1]。體外研究ADAR1-IN-1(CompoundC12)(1-3μM,1-4days)significantlyinhibitsthegrowthandcolonyformationofDU-145cellsataconcentrationof1μM,withmaximalinhibitionobservedat3μM[1].ADAR1-IN-1(1-3μM,24h)dose-dependentlyinhibitsthemigrationandinvasionofDU-145cellsby[1].ADAR1-IN-1(1-3μM,24-48h)significantlyarrestsDU-145cellsintheG0/G1phaseandinducesapoptosisinadose-dependentmanner[1].ADAR1-IN-1(1-3μM,48h)inducesadownregulationofN-cadherinandvimentinandaupregulationofp53[1].ADAR1-IN-1(72h)exhibitssignificantproliferationinhibitionagainstandrogenreceptor-dependentVCaPcells,castration-resistant22Rv1cells,andAR-negativePC-3cellswithIC50valuesof1.76μM,1.79μM,and0.72μM,respectively[1].CellMigrationAssay[1]CellLine:DU-145cellsConcentration:1,2and3μMIncubationTime:24hResult:Dose-dependentlyinhibitedthemigration.1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemECellCycleAnalysis[1]CellLine:DU-145cellsConcentration:1,2and3μMIncubationTime:24hResult:ArrestedcellsintheG0/G1phase.ApoptosisAnalysis[1]CellLine:DU-145cellsConcentration:1,2and3μMIncubationTime:24hResult:Inducedapoptosisinadose-dependentmanner.WesternBlotAnalysis[1]CellLine:DU-145cellsConcentration:1,2and3μMIncubationTime:48hResult:Inducedaconcentration-dependentdownregulationofN-cadherinandvimentin.DecreasedCDk6andc-MYC,andincreasedp53.體內(nèi)研究ADAR1-IN-1(CompoundC12)(15-30mg/kg,i.p.,twicedailyfor19days)haspotentantitumorefficacyandsafetypropertiesinDU-145and22Rv1xenograftmicemodels[1].AnimalModel:DU-145and22Rv1xenograftmodelsestablishedinmaleBALB/cnudemice[1]Dosage:15and30mg/kgAdministration:Intraperitonealinjection(i.p.),twicedailyfor19daysResult:Significantlyinhibitedtumorgrowthwithtumorgrowthinhibition(TGI)ratesof41.8%and52.8%,respectivelyinDU-145modeland46.4%and59.0%,respectivelyin22Rv1model.Noobviouslesionswereobservedinthemainorgansofthemice.REFERENCES2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEZhuY,etal.Design,Synthesis,andActivityEvaluationofNovelNucleosidesasADAR1InhibitorfortheTreatmentofProstateCancer.JMedChem.2025Jul24;68(14):14495-14513.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical