Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEPROTACPI3K/110βdegrader-2Cat.No.:HY-174469CASNo.:3070438-79-5分子式:C??H??N?O?S分子量:948.18作用靶點(diǎn):PROTACs;P-glycoprotein;Apoptosis;ReactiveOxygenSpecies(ROS);Akt;Bcl-2Family;Na+/K+ATPase;PI3K作用通路:PROTAC;MembraneTransporter/IonChannel;Apoptosis;Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB;PI3K/Akt/mTOR儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性PROTACPI3K/110βdegrader-2是一種選擇性PI3K/p110βPROTAC降解劑。PROTACPI3K/110βdegrader-2可以顯著降解110β蛋白并抑制P-糖蛋白的表達(dá)。PROTACPI3K/110βdegrader-2可以增加活性氧(ROS)的水平。PROTACPI3K/110βdegrader-2通過激活內(nèi)質(zhì)網(wǎng)應(yīng)激(ERS)介導(dǎo)的線粒體凋亡apoptosis通路和抑制AKT/Bcl-2信號通路發(fā)揮抗腫瘤作用。PROTACPI3K/110βdegrader-2可用于癌癥的研究。(粉色:PI3K/110β配體(HY-75124);藍(lán)色:VHL配體(HY-125845);黑色:連接子(HY-W002042))[1]。IC50&TargetPI3KBaxBcl-2Akt體外研究PROTACPI3K/110βdegrader-2(CompoudJ-6)(24h)hassignificantanti-tumoractivityinA549(IC50=58.2μM),A549/DDP(IC50=39.23μM),MCF-7(IC50=53.99μM)andMCF-7/ADM(IC50=38.73μM)cells[1].PROTACPI3K/110βdegrader-2(0-50μM,0-48h)canselectivelydegrade110βproteininMCF-7/ADMandA549/DDPcellsinatimeandconcentration-dependentmanner[1].PROTACPI3K/110βdegrader-2(0-25μM,24h)significantlyincreasesROSlevels,reducesmitochondrialmembranepotential,andactivatesERSmediatedapoptosisinMCF-7/ADMandA549/DDPcells[1].PROTACPI3K/110βdegrader-2(0-25μM,24h)inhibitsNa+/K+-ATPaseactivityandreducesP-GlycoproteinexpressioninMCF-7/ADMandA549/DDPcells[1].ApoptosisAnalysis[1]CellLine:MCF-7/ADMandA549/DDPcells1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEConcentration:6.25,12.5and25μMIncubationTime:24hResult:SignificantlyincreasedtheproportionofcellapoptosisandthelevelofCaspase3,Cyt-3andCaspase12.WesternBlotAnalysis[1]CellLine:MCF-7/ADMandA549/DDPcellsConcentration:25μMIncubationTime:24hResult:IncreasedtheproteinlevelofP-PERK,ATF4,CHOP,.PTENandBAXanddecreasedtheproteinlevelofP-AKTandBcl-2.WesternBlotAnalysis[1]CellLine:MCF-7/ADMandA549/DDPcellsConcentration:0.25,2.5and25μMIncubationTime:24hResult:SignificantlyreducedthelevelofP-Glycoprotein.體內(nèi)研究PROTACPI3K/110βdegrader-2(CompoudJ-6)(50mg/kg;i.p.;onceeveryotherday;7times)effectivelyinhibitsthegrowthoftumorbydegrading110βproteinintheMCF-7/ADMinjectedfemaleBALB/cmice[1].AnimalModel:FemaleBALB/cmice(5-6weeks)bearingMCF-7/ADMxenografttumor[1]Dosage:50mg/kgAdministration:Intraperitonealinjection(i.p.);onceeveryotherdayfor7timesResult:Significantlyreducedtumorvolume.Effectivelydownregulatedthelevelof110βintumortissue.SignificantlyincreasedthelevelofATF6,CHOP,GRP78,Caspase-12andBAXinhibitedcaspase-8,P-AKT,Bcl-2andP-Glycoprotein.Didnotsignificantlyaffectweightanddidnotcauseorgandamage.REFERENCES[1].CenJ,etal.DoubleSwordsinOne:NovelSelectivePI3K/110βPROTACDegradersfortheTreatmentofMultidrug-ResistantCancerby2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEActivatingERSandInhibitingP-gp.JMedChem.2025May8;68(9):9446-9464.McePdfHeightCaution:Producthasnotbeenfully