A2AAR-HDAC-IN-2-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEA2AAR/HDAC-IN-2Cat.No.:HY-143325CASNo.:2767560-94-9分?式:C??H??N?O?分?量:450.49作?靶點(diǎn):HDAC;AdenosineReceptor作?通路:CellCycle/DNADamage;Epigenetics;GPCR/GProtein儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性A2AAR/HDAC-IN-2?種有效的A2AAR/HDAC雙重抑制劑，其對(duì)A2AAR具有良好的親和?(Ki=10.3nM),對(duì)HDAC1具有良好的抑制活性(IC50=18.5nM).A2AAR/HDAC-IN-2可?于抗腫瘤的研究。IC50&TargetHDAC1HDAC2HDAC3HDAC618.5nM(IC50)16.0nM(IC50)13.6nM(IC50)2.1nM(IC50)HDAC8A1ARA2AARA2BAR1408.9nM(IC50)105.6nM(Ki)10.3nM(Ki)513.0nM(Ki)A3AR＞10μM(IC50)體外研究A2AAR/HDAC-IN-2(compound30c)(5nM-100μM;72h)showsanti-proliferativeactivity,withGI50sof12.16and12.61μMforCT26andMC38cells,respectively[1].A2AAR/HDAC-IN-2(0.1,1,5,10μM;24h)increaseshistoneH3andH4acetylationinaconcentration-dependentmannerinMC38cells[1].CellProliferationAssay[1]CellLine:MC38andCT26cellsConcentration:5nM-100μMIncubationTime:72h1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:Showedgoodanti-proliferativeactivityincancercelllines,withGI50sof12.16and12.61μMforCT26andMC38cells,respectively.WesternBlotAnalysis[1]CellLine:MC38cellsConcentration:0.1,1,5,10μMIncubationTime:24hResult:SignificantlyincreaseshistoneH3andH4acetylationat10μMandinaconcentration-dependentmanner.REFERENCES[1].ZhangJ,etal.Dual-actingantitumoragentstargetingtheA2Aadenosinereceptorandhistonedeacetylases:Designandsynthesisof4-(furan-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-aminederivatives.EurJMedChem.2022Jun5;236:114326.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;