Bortezomib-GMP-PS-341-GMP-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEBortezomib(GMP)Cat.No.:HY-10227GSynonyms: PS-341(GMP);LDP-341(GMP);NSC681239(GMP)分子式: C₁₉H₂₅BN₄O₄分子量: 384.24作用靶点: Proteasome;NF-κB;Apoptosis;Autophagy作用通路: MetabolicEnzyme/Protease;NF-κB;Apoptosis;Autophagy储存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Bortezomib(GMP)(PS-341(GMP))是GMP级别的Bortezomib(HY-10227)。GMP级别的小分子可用做细胞疗法中的辅助试剂。Bortezomib(PS-341)是一种可逆性和选择性的蛋白酶体(proteasome)抑制剂，通过靶向苏氨酸残基有效抑制20S蛋白酶体(Ki=0.6nM)。Bortezomib破坏细胞周期、诱导细胞凋亡以及抑制核因子NF-κB。Bortezomib是第一种蛋白酶体抑制剂，具有抗癌活性。体外研究Bortezomib(GMP)(PS-341(GMP))(100nM;8hours)resultsintheaccumulationofcellsinG2-M,withacorrespondingdecreaseinthenumberofcellsinG1[1].Bortezomib(GMP)(5-100nM;20hours)inducesapoptosisinmantle-celllymphoma(MCL)celllines[3].Bortezomib(GMP)(20nM;1-14hours)inducesNoxaup-regulationinbothMCLcelllines[3].TheIC50ofBortezomib(GMP)isfoundtobe2.46nMfor26SproteasomeintheB16F10cells[4].Bortezomib(GMP)suppressesseveralanti-apoptoticproteins(e.g.,Bcl-XL,Bcl-2,andSTAT-3)[5].CellCycleAnalysis[1]CellLine:PC-3cellsConcentration:100nMIncubationTime:8hoursResult:ResultedintheaccumulationofcellsinG2-M,withacorrespondingdecreaseinthenumberofcellsinG1.CellViabilityAssay[3]1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemECellLine:JVM-2,Granta-519,Jeko,REC-1cells(MCLcelllines)Concentration:5-100nMIncubationTime:20hoursResult:ThemedianLD50fortheseMCLcelllineswas31nM(range,18.2-60.1nM).WesternBlotAnalysis[3]CellLine:wtp53(Granta-519),mutp53(Jeko)cellsConcentration:20nMIncubationTime:1,2,4,6,14hoursResult:Noxaup-regulationwasdetectedbetween2to4hoursafterbortezomib(PS-341).体内研究Bortezomib(GMP)(PS-341(GMP))(0.3-1mg/kg;i.v.;onceweeklyfor4weeks)inhibitsPC-3TumorGrowthinNudeMice[1].AnimalModel:Malenudemice(xenografttumormodelbearingPC-3cells)[1]Dosage:0.3,1mg/kgAdministration:Intravenousinjection;onceweeklyfor4weeksResult:Resultedinasignificantdecreaseintumorgrowth~60%atdoseof1mg/kg.客户使用本产品发表的科研文献SignalTransductTargetTher.2025Apr23;10(1):131.Cell.2019Jul11;178(2):330-345.e22.CancerDiscov.2025Jun16.NatCancer.2020Feb;1(2):235-248.NatImmunol.2023Mar;24(3):531-544.Seemorecustomervalidationsonwww.MedChemEREFERENCESAdamsJ,etal.Proteasomeinhibitors:anovelclassofpotentandeffectiveantitumoragents.CancerRes.1999Jun1;59(11):2615-22.ShahshahanMA,etal.Potentialusageofproteasomeinhibitorbortezomib(Velcade,PS-341)inthetreatmentofmetastaticmelanoma:basicandclinicalaspects.AmJCancerRes.2011;1(7):913-24.2/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEPérez-GalánP,etal.Theproteasomeinhibitorbortezomibinducesapoptosisinmantle-celllymphomathroughgenerationofROSandNoxaactivationindependentofp53status.Blood.2006Jan1;107(1):257-64.YerlikayaA,etal.CombinedeffectsoftheproteasomeinhibitorbortezomibandHsp70inhibitorsontheB16F10melanomacellline.MolMedRep.2010Mar-Apr;3(2):333-9.MujtabaT,etal.Advancesintheunderstandingofmechanismsandtherapeuticuseofbortezomib.DiscovMed.2011Dec;12(67):471-80.FernándezY,etal.Chemicalblockageoftheproteasomeinhibitoryfunctionofbortezomib:impactontumorcelldeath.JBiolChem.2006Jan13;281(2):1107-18.McePdfHeightCaution:Producthas