Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBcl-2-IN-8Cat.No.:HY-144819分?式:C??H??O?分?量:572.73作?靶點(diǎn):Apoptosis;Bcl-2Family作?通路:Apoptosis儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Bcl-2-IN-8?種有效的抗癌劑。Bcl-2-IN-8對(duì)藥物敏感和耐藥的癌細(xì)胞均顯?抗增殖活性。Bcl-2-IN-8誘導(dǎo)細(xì)胞凋亡(apoptosis)和細(xì)胞周期停滯在G1期。Bcl-2-IN-8以劑量依賴(lài)性?式抑制細(xì)胞遷移。Bcl-2-IN-8具有三乳腺癌的研究潛?[1]。IC50&TargetBaxBcl-2體外研究Bcl-2-IN-8(compound4m)(48h)showsselectivecytotoxicityagainstMDA-MB-231,MCF-7/ADR,MCF-10AcellswithIC50sof0.51,0.38,3.56μM,respectively[1].Bcl-2-IN-8(0-8μM;24,48,72h)inhibitscellproliferationinadose-timedependently[1].Bcl-2-IN-8(0-2μM;24h)inducescellcyclearrestatG1phaseinMDA-MB-231cells[1].Bcl-2-IN-8(0-2μM;24h)inducesapoptosisinMDA-MB-231cells[1].Bcl-2-IN-8(0-3μM;24h)up-regulatestheexpressionofBax,cytochromecanddown-regulatesBcl-2,P53proteininaconcentrationdependentlyinMDA-MB-231cells[1].Bcl-2-IN-8(0-3μM;24h)decreasestheΔΨmandinducesROS(reactiveoxygenspecies)generationbyactivatingthep38MAPK-AktsignalingpathwayinMDA-MB-231cells[1].Bcl-2-IN-8(0-2μM;24h)increasesintracellularCa2+concentrationfrom9.9treatedwithDMSOto37.4treatedat2μMinMDA-MB-231cells[1].Bcl-2-IN-8(0-3μM;24h)significantlyinhibitsmigrationinadose-dependentmannerinMDA-MB-231cells[1].Bcl-2-IN-8(0-3μM;24h)increasestheexpressionlevelsofSmad7butdecreasestheexpressionlevelsofp-Smad3inMDA-MB-231cells[1].CellCytotoxicityAssay[1].1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:MB-231,MCF-7,MCF-7/adriamycin(adriamycin-resistantMCF-7cellline)cellsConcentration:IncubationTime:48hResult:ShowedpotentinhibitoryactivitiesonMDA-MB-231,MCF-7,MCF-7/ADR(adriamycin)cellswithIC50sof0.51,2.01,0.38μM,respectively.CellProliferationAssay[1].CellLine:MDA-MB-231cellsConcentration:0-8μMIncubationTime:24,48,72hResult:Inhibitedcellproliferationinadose-timedependently.CellCycleAnalysis[1].CellLine:MDA-MB-231cellsConcentration:0.5,1,2μMIncubationTime:24hResult:Arrestedthecell-cycleattheG1phaseandthepercentageofcellsintheG1phasefrom54.8to74.6%.WesternBlotAnalysis[1].CellLine:MDA-MB-231cellsConcentration:0.5,1,2,3μMIncubationTime:24hResult:DecreasedtheexpressionofcyclinD1,CDK4andCDK6protein,butdidnotinfluencetheexpressionofc-mycproteins.ApoptosisAnalysis[1].CellLine:MDA-MB-231cellsConcentration:0,0.5,1,2μMIncubationTime:24h2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:Thetotalpercentageofearlyandlateapoptosisincreasedto10.2%,17.6%,56.4%withtheconcentrationof0.5μM,1μM,2μM.體內(nèi)研究Bcl-2-IN-8showsmetabolicstabilitywithCL50valueof14.1mL/min/mgandremaining(T=100min)of18.5%inrats[1].REFERENCES[1].LiangJJ,etal.Synthesisandstructure-activityrelationshipstudyofapotentMHO7analogueaspotentialanti-triplenegativebreastcanceragent.EurJMedChem.2022Jun5;236:114313.McePdfHeightCaution:Producthasnotbeenfullyvali