Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPARP1-IN-12Cat.No.:HY-150765分?式:C??H??FN?O?分?量:741.93作?靶點:PARP;Apoptosis作?通路:CellCycle/DNADamage;Epigenetics;Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性PARP1-IN-12?種有效的PARP1抑制劑，其IC50值為2.99nM。PARP1-IN-12具有較好的抗癌細胞增殖活性，可誘導細胞凋亡并使細胞周期停滯在G2/M期。PARP1-IN-12能在BRCA缺陷的細胞中誘導DNA雙鏈斷裂(DSBs)。IC50&TargetPARP-12.99nM(IC50)體外研究PARP1-IN-12(compound20e)(0.1,0.3,1μM;48h)exhibitsactivitiesofantiproliferationandselectivelykillingBRCA-deficientcells,canalsoinduceDNAdoublestrandbreaks(DSBs)inBRCA-deficientcellsinaconcentration-dependentmanner[1].PARP1-IN-12(10μM,48h)enhancestheproteinlevelsofphosphorylatedChk1[1].PARP1-IN-12(1,3,10μM;48h)activatscellcyclecheckpoints,theninducesG2/MarrestinBRCA-deficientcellsand(1,5,10μM;96h)alsoinducesMDA-MB-436cellsapoptosisinaconcentration-dependentmanner[1].CellProliferationAssay[1]CellLine:UWB1.289(BRCA1-deficient),UWB1.289+BRCA1(BRCA1restored),MDA-MB-436(BRCA1-deficient),Capan-1(BRCA2-deficient)cellsConcentration:0.1,0.3,1μMIncubationTime:48hResult:ShowedantiproliferativeactivitywithIC50sof0.27,1.43,0.87,0.19μMforUWB1.289,1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEUWB1.289+BRCA1,Capan-1andMDA-MB-436cells,respectively.Immunofluorescence[1]CellLine:MDA-MB-436,Capan-1cellsConcentration:10μMIncubationTime:48hResult:EnhancedtheproteinlevelsofphosphorylatedChk1butthelevelsofcorrespondingtotalproteinswerenotaltered.CellCycleAnalysis[1]CellLine:Capan-1cellsConcentration:1,3,10μMIncubationTime:48hResult:InducedG2/MarrestinBRCA-deficientcellsinaconcentration-dependentmanner.ApoptosisAnalysis[1]CellLine:MDA-MB-436cellsConcentration:1,5,10μMIncubationTime:96hResult:Causedapoptosisinaconcentration-dependentmannerinMDA-MB-436cells.WesternBlotAnalysis[1]CellLine:MDA-MB-436,Capan-1cellsConcentration:0.1,0.3,1μMIncubationTime:48hResult:InducedincreasedlevelsofγH2AXinaconcentration-dependentmannerinbothMDA-MB-436andCapan-1cells.REFERENCES[1].KayumovM,etal.Design,synthesisandpharmacologicalevaluationofnewPARP1inhibitorsbymergingpharmacophoresofolaparibandthenaturalproductalantolactone.EurJMedChem.2022Jun28;240:114574.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.