Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBRD4Inhibitor-18Cat.No.:HY-146660CASNo.:2451219-73-9分?式:C??H??ClN?O?S分?量:496.02作?靶點:c-Myc;EpigeneticReaderDomain;Apoptosis作?通路:Apoptosis;Epigenetics儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性BRD4Inhibitor-18?種?效的BRD4抑制劑，IC50為110nM。BRD4Inhibitor-18具有疏??酰環(huán)戊側鏈。BRD4Inhibitor-18能顯著抑制BRD4?平較?的MV-4-11細胞的增殖，具有促進細胞凋亡(apoptosis)和抑制G0/G1周期的活性[1]。IC50&TargetBRD4110nM(IC50)體外研究BRD4Inhibitor-18(compound13f)(0-10μM;72hours)cansuppresstheproliferationofHL-60andMV-41cells[1].BRD4Inhibitor-18(0.5and5μM;12hours)significantlyarrestsMV-4-11cellsinG1phaseinadose-dependentmanner[1].BRD4Inhibitor-18(0.5and5μM;12hours)effectivelyinducesapoptosisofMV-4-11cellsinadose-dependentmanner[1].BRD4Inhibitor-18(0.5and5μM;4hours)inhibitstheexpressionofc-Mycproteininadose-dependentmanner[1].CellProliferationAssayCellLine:HL-60andMV-4-11[1]Concentration:0-10μMIncubationTime:72hours1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:SuppressedtheproliferationofHL-60andMV-41cellswithIC50sof5.52μMand0.42μM.CellCycleAnalysisCellLine:MV-4-11cells[1]Concentration:0.5and5μMIncubationTime:12hoursResult:SignificantlyarrestedMV-4-11cellsinG1phase,withtheG0/G1cellproportionsof50.87%and70.66%at0.5and5μM.ApoptosisAnalysisCellLine:MV-4-11cells[1]Concentration:0.5and5μMIncubationTime:12hoursResult:EffectivelyinducedapoptosisofMV-4-11cells,withapoptosisratesof12.39%and73.24%atat0.5and5μM.WesternBlotAnalysisCellLine:MV-4-11cells[1]Concentration:0.5and5μMIncubationTime:4hoursResult:Inhibitedtheexpressionofc-Mycproteininadose-dependentmanner.REFERENCES[1].LiQ,LiJ,CaiY,etal.Design,synthesisandbiologicalevaluationofnovel6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-onederivativesaspotentialBRD4inhibitors.BioorgMedChem.2020;28(15):115601.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonl