Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemENogo-B-IN-1Cat.No.:HY-175317分子式: C??H??Cl?N?O?分子量: 605.89作用靶點(diǎn): PI3K;Akt;NF-κB;Bcl-2Family;Apoptosis作用通路: PI3K/Akt/mTOR;NF-κB;Apoptosis儲(chǔ)存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Nogo-B-IN-1((S,R)-4v)是一種共價(jià)Nogo-B抑制劑。Nogo-B-IN-1通過抑制Nogo-B活性和PI3K/AKT/NF-κB/Bcl-2信號(hào)通路來抑制骨肉瘤(OS)的進(jìn)展。Nogo-B-IN-1抑制OS143B細(xì)胞的增殖(IC50=0.28μM)，誘導(dǎo)細(xì)胞凋亡(apoptosis)。Nogo-B-IN-1可用于OS靶向研究[1]。體外研究Nogo-B-IN-1(0-3μM,24h)inhibitsthemigrationandproliferation,inducesabnormalcellmorphology,cellularshrinkage,disorderedarrangement,apoptosisdependsonNogo-Bin143Bcells[1].Nogo-B-IN-1(50μM)inhibitsNogo-Bexpression,withinhibitoryactivityof99%in143Bcells[1].Nogo-B-IN-1(0-3μM,24h)canbluntNogo-B,whichinturnimpairsPI3K/AKTandNF-κBactivitiesin143Bcells[1].CellMigrationAssay[1]CellLine:143BcellsConcentration:0nM,300nM,1000nMIncubationTime:24hResult:Decreasedthepercentageofintercellularwoundhealingdistance,decreasedthecolonygrowth.ApoptosisAnalysis[1]CellLine:143BcellsConcentration:0nM,300nM,1000nM1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEIncubationTime:24hResult:Inducedapoptosis.WesternBlotAnalysis[1]CellLine:143BcellsConcentration:0,0.3,0.5,1,3μMIncubationTime:0,24,48,72hResult:DownregulatedNogo-Bproteinlevel,enhancedthestabilityofNogo-B.Decreasedp65,Bcl-2protein,inhibitedactivationofPI3K,AKT,andp-AKT.RT-PCR[1]CellLine:143BcellsConcentration:0,0.3,0.5,1,3μMIncubationTime:24hResult:HadnoeffectofNogo-BmRNAlevel.體內(nèi)研究Nogo-B-IN-1(30mg/kg,i.p.,onceaday,23days)suppressesOSprogressionwithoutobvioustoxicityin143BxenograftBALB/cnudemicemodel[1].Nogo-B-IN-1(30mg/kg,i.p.,onceaday,23days)isweakenedtheinhibitoryeffectoftumorvolumeandtumorweightin43BwithNogo-BknockdownxenograftBALB/cnudemicemodel[1].AnimalModel:143B(5×106)xenograftBALB/cnudemice(3-month-old)model[1]Dosage:30mg/kgAdministration:i.p.,onceaday,23daysResult:Suppressedtumorgrowth,hadnodiscerniblemorphologicalchangesintheheart,liver,spleen,orkidneytissues.AnimalModel:143B(5×106)withNogo-BknockdownxenograftBALB/cnudemice(3-month-old)model[1]Dosage:30mg/kgAdministration:i.p.,onceaday,23daysResult:Wasweakenedtheinhibitoryeffectoftumorvolumeandtumorweight.2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEREFERENCESXueJ,LiM,KangL,WangM,YinJ,SunD,DengY,WeiQ,WongJ,ZhuT,LiuS.IdentificationofNogo-Basapotentialtherapeutictargetofosteosarcomaviastereochemicallyselectivecovalentprobes.CellDeathDis.2025Jul19;16(1):537.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical