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Medchemexpress/Bafilomycin A1(Synonyms: (-)-Bafilomycin A1)/HY-100558/10mM*1mL in DMSO
Description | BafilomycinA1isamacrolideantibioticisolatedfromtheStreptomycesspeciesandaninhibitorofvacuolarV-ATPase. |
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InVitro | BafilomycinA1atalowconcentration(1nM)effectivelyandspecificallyinhibitsandkillspediatricB-cellacutelymphoblasticleukemiacells.Ittargetsbothearlyandlatestagesoftheautophagypathway,mitochondriaandinducescaspase-independentapoptosis.BafilomycinA1inducesthebindingofBeclin1toBcl-2,whichfurtherinhibitsautophagyandpromotesapoptoticcelldeath[1].ThegrowthoftheBEL-7402hepatocellularcarcinomaandHO-8910ovariancancercelllinesareretardedandthemetastaticpotentialisinhibitedbybafilomycinA1.Transmissionelectronmicroscopyandassaysofcapsase-3and−9suggestthatbafilomycinA1inducesapoptosis[2].BafilomycinA1inhibitsthegrowthofavarietyofculturedcellsdose-dependently,includinggoldenhamsterembryoandNIH-3T3fibroblasts,whetherornottheyaretransformed,andPC12andHeLacells.TheIC50ofbafilomycinA1forinhibitionofcellgrowthrangesfrom10to50nM[3]. |
InVivo | Chronictreatmentwithlow-dosebafilomycinA1(0.1mg/kg)slightlyinhibitsthetumorvolume,butthefinaltumorvolumedoesnotdiffersignificantlyfromthecontrol.However,chronictreatmentwithhighdosebafilomycinA1(1mg/kg)inhibitsthetumorgrowthsignificantly,comparedwithcontrols,after21days[4]. |
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CellAssay [2] | Cellsareharvestedusing0.05%trypsinandsUSPendedinculturemediumcontaining10%FCS,and200µLsuspensionisaddedtoeachwellofa96-wellplate.Cellsareculturedfor20hforadhesion.BafilomycinA1isaddedtothewellsatthefinalconcentrationsof200,400and800nM,intriplicate.At24,48and72h,20µlWST-1isaddedtothecells.Followingincubationat37°Cfor4h,theplatesarereadtodeterminetheopticaldensity(OD)at435nmwith675nmreferenceusingaspectrophotometer[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly. AnimalAdmiNISTration | [2] Mouse:Tumor-bearingmicearedividedrandomlyintothreeexperimentalgroups:alow-dosebafilomycinA1(0.1mg/kgperday)-treatedgroup(n=5),ahigh-dosebafilomycinA1(1mg/kgperday)-treatedgroup(n=5),andacontrolgroup(n=5).Tumorsizeismeasuredandtumorvolumedoublingtimeiscalculated[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly. References |
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