Huib32-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEHuib32Cat.No.:HY-178124分子式: C₁₆H₂₃N₅O₄S分子量: 381.45作用靶点: Deubiquitinase作用通路: CellCycle/DNADamage储存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性 Huib32是一种高效的小分子USP32抑制剂(IC50=21.2nM)，相较于其他密切相关的去泛素化酶(DUBs)(例如USP8/10/16、UCHL1和OTUB2)具有高选择性。Huib32通过可逆地共价结合活性位点Cys743来抑制USP32，从而增强底物的泛素化水平、改变内体形态，并模拟USP32敲除的表型。Huib32可用于乳腺癌、卵巢癌、肺癌，阿尔茨海默病和帕金森病的相关研究[1]。IC50&TargetUSP3221.2nM(IC50)体外研究Huib32(BB01CA282)(0-50μM,6-24h)selectivelyinhibitsbothUSP32FLandUSP32CDinadose-dependentmanner(from0.1μM),withnosignificanteffecton16otherdetectedDUBs[1].Huib32(0-50μM,24h)demonstratespotent,dose-dependenttargetengagementofendogenousUSP32inMelJuSocells(IC50~0.1μM),confirmingitscellpermeabilityandcellularon-targetactivity[1].Huib32(10μM,4-72h)induceslateendosomedispersionandenhancesubiquitinationofRAB7andothersubstrates(e.g.,RAB6,RAB32,RAB11A/B,TMEM192),confirmingitsroleinmembranetraffickingandrevealingnewpotentialsubstratesofUSP32[1].Huib32(10μM,4-72h)significantlyalterstheubiquitinome,enrichinganddepletinguniqueLys-ε-Gly-Glypeptidesat4hand72h,impactingsubstrateslikeRAB11A/BandUSP32itselfwithoutchangingtheirtotalproteinlevels,indicatingnon-proteolyticubiquitination[1].Huib32(10μM,72h)specificallyincreasedtheubiquitinationofGFP-RAB7WT,butnottheGFP-RAB72KRmutant,validatingitson-targeteffectagainstanestablishedUSP32substrate[1].WesternBlotAnalysis[1]CellLine:MelJuSocells1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEConcentration:0,0.1,0.5,1,5,10,and50μMIncubationTime:4,24and72hResult:StronglyincreasedtheubiquitinationofRAB7after4hofincubationinMelJuSocellsstablyexpressingGFP-RAB7,whichsteadilystayedupto72hofincubation.Approximately2-foldincreaseinRAB7ubiquitinationwasobservedinGFP-RAB7WT,butnotintheubiquitination-deficientmutantGFP-RAB72KR.Immunofluorescence[1]CellLine:MelJuSocellsConcentration:0,5and10μMIncubationTime:72hResult:Induceddispersionandswellingofthelateendosomalcompartments,aphenotypeconsistentwithUSP32depletion.REFERENCESScherpe,S.,etal.Huib32:APotentandSelectiveUSP32InhibitorModulatingEndosomalProcessesandAdvancingCell-PermeableUSP32Probes.bioRxiv(2025).McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Fo