Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEApogossypoloneCat.No.:HY-19551CASNo.:886578-07-0Synonyms:ApoG2分?式:C??H??O?分?量:490.5作?靶點:Bcl-2Family;Apoptosis;Autophagy;Fungal;ROSKinase作?通路:Apoptosis;Autophagy;Anti-infection;ProteinTyrosineKinase/RTK儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Apogossypolone(ApoG2)?種具有?服活性的Bcl-2familyproteins抑制劑，對Bcl-2,Mcl-1和Bcl-XL的Ki值分別為35,25和660nM。Apogossypolone具有抗腫瘤活性，誘導細胞凋亡(apoptosis)[1]和?噬(autophagy)[2]。Apogossypolone具有抗真活性[3]。IC50&TargetMcl-1Bcl-2Bcl-xL25nM(Ki)35nM(Ki)660nM(Ki)體外研究Apogossypolone(ApoG2)showsimprovedstabilityunderstressedconditions[1].Apogossypolone(0-1μM,72or96h)inhibitsWSU-DLCL2cellsgrowthinadose-dependentmanner[1].Apogossypolone(0-5μM,24or48h)interfereswiththeformationofheterodimersbetweenanti-apoptoticandpro-apoptoticBcl-2familymembers,andleadstocleavageofcaspase-3,caspase-9andPARP[1].Apogossypolone(0-8μM,0-72h)inducesapoptoticWSU-DLCL2celldeathinatime-anddose-dependentmanner[1].Apogossypolone(0-10μM,0-24h)inducesautophagyandpromotesROSgenerationinHCCcells[2].CellProliferationAssay[1]CellLine:WSU-DLCL2Concentration:250,350,500and1000nMIncubationTime:96hforcellcounting,72hforMTT1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:Inhibitedgrowthinadose-dependentmanner.The50%growthinhibitionconcentration(IC50)wasapproximately350nM.WesternBlotAnalysis[1]CellLine:WSU-DLCL2Concentration:0.35,0.5,1and5μMIncubationTime:24or48hResult:BlockedtheformationofheterodimersbetweenBcl-XLandBiminaconcentration-dependentmanner.Resultedintheactivationofcleavagesofcaspase-3,caspase-9andPARP.ApoptosisAnalysis[1]CellLine:WSU-DLCL2Concentration:0,1,2,4and8μMIncubationTime:24,48and72hResult:Inducedcellapoptosisinatime-anddose-dependentmanner.CellAutophagyAssay[2]CellLine:HepG2andHep3BConcentration:1.25,2.5,5and10μMIncubationTime:6,12,18and24hResult:InducedLC3(Lightchain3)-IIconversioninadose-andtime-dependentmanner.體內(nèi)研究Apogossypolone(ApoG2)(120mg/kg;i.v.orp.o.;onceadayfor5days)effectivelyinhibitsgrowthofdiffuselargecelllymphomacellswithouttoxicity[1].AnimalModel:Four-week-oldfemaleICR-SCIDmice,eachmousereceived107WSU-DLCL2cells(inserum-freeRPMI1640)subcutaneously(sc)ineachflankarea[1]Dosage:120mg/kgAdministration:IntravenousoradministrationperdayforfivedaysResult:InhibitedthegrowthofWSU-DLCL2andsignificantlydecreasedthetumorweight.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:Non-tumor-bearingSCIDmice[1]Dosage:160mg/kgAdministration:IntravenousoradministrationperdayforfivedaysResult:Waswelltoleratedinmiceupto800mg/kg.Displayednogrosssignsoftoxicity.REFERENCES[1].YuanSun,etal.Apogossypolone,anonpeptidicsmallmoleculeinhibitortargetingBcl-2familyproteins,effectivelyinhibitsgrowthofdiffuselargecelllymphomacellsinvitroandinvivo.CancerBiolTher.2008Sep;7(9):1418-26.[2].JayEMellon,etal.Inhibitoryeffectsofgossypol,gossypolone,andapogossypoloneonacollectionofeconomicallyimportantfilamentousfungi.JAgricFoodChem.2012Mar14;60(10):2740-5.[3].ChengP,etal.ThenovelBH-3mimeticapogossypoloneinducesBeclin-1-andROS-mediatedautophagyinhumanhepatocellularcarcinoma[corrected]cells.CellDeathDis.2013Feb7;4(2):e489.McePdfHeightCaution:Produc