SARS-CoV-2-nsp14-IN-10-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESARS-CoV-2nsp14-IN-10Cat.No.:HY-179556分⼦式:C₂₄H₂₂F₃N₇O₃S分⼦量:545.54作⽤靶点:SARS-CoV作⽤通路:Anti-infection储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性SARS-CoV-2nsp14-IN-10⼀种⾼效且选择性极⾼的NSP14(IC50=0.34µM)S-腺苷甲硫氨酸(SAM)结合⼝袋抑制剂。SARS-CoV-2nsp14-IN-10对SARS-CoV-2具有显著的抗病毒活性。SARS-CoV-2nsp14-IN-10对其他β冠状病毒也具有⼴谱活性，并能在复制阶段抑制SARS-CoV-2。SARS-CoV-2nsp14-IN-10可抑制病毒翻译并具有免疫刺激作⽤。SARS-CoV-2nsp14-IN-10可特异性逆转NSP14介导的宿主转录组改变。SARS-CoV-2nsp14-IN-10可⽤于SARS-CoV-2的研究[1]。体外研究SARS-CoV-2nsp14-IN-10(CompoundC10)(20-500µM)specificallybindstotheSAMrecognitionpocketofNSP14(KD=187nM)inacompetitivemannerwithSAM[1].SARS-CoV-2nsp14-IN-10(5-25μM,8h)enhancesthethermostabilityofNSP14proteininHEK293-NSP14cells,indicatingthatitbindstothetargetinlivingcells[1].SARS-CoV-2nsp14-IN-10(24h)significantlyreducestheinfectionratesoftheoriginalSARS-CoV-2strain,Delta,andOmicronvariantsinA549-ACE2cells(EC50valuesof0.31μM,0.50μMand0.06μM,respectively)[1].SARS-CoV-2nsp14-IN-10(10µM,24h)potentlyinhibitsthereplicationphaseofSARS-CoV-2inHeLacells[1].SARS-CoV-2nsp14-IN-10(3-20μM,0-24h)showsstronginhibitoryactivityinA549-ACE2cellsinfectedwithSARS-CoV-2trVLPduringbothfull-timeandpost-entrytreatments,whileentrytreatmentshowsnosignificantinhibition[1].SARS-CoV-2nsp14-IN-10(20-40μM,8h)inhibitsthetranslationinitiationofSARS-CoV-2mRNAinA549-ACE2cellsinfectedwithtrVLP,specificallybycapmaturation,selectivelyimpairing[1].SARS-CoV-2nsp14-IN-10(20-40µM,8h)selectivelyinhibitsviraltranslationinA549-ACE2cellsinfectedwithSARS-CoV-2trVLP[1].SARS-CoV-2nsp14-IN-10(20μM,24h)significantlyreducedtheexpressionlevelsofSpikemRNAand1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEproteininA549-ACE2cellsinfectedwithSARS-CoV-2trVLP[1].SARS-CoV-2nsp14-IN-10(20μM,24h)upregulatestheexpressionofinterferon-stimulatedgenes(ISGs)suchasRSAD2,IFI6,andIRF7inA549-ACE2cells[1].SARS-CoV-2nsp14-IN-10(5-20μM,48h)reverseshosttranscriptomechangesinducedbyNSP14expressioninHEK293-NSP14cells[1].WesternBlotAnalysis[1]CellLine:HEK293-NSP14cellsConcentration:5μM,10μM,15μM,20μM,25μMIncubationTime:8hResult:EnhancedthethermalstabilityofNSP14protein.体内研究SARS-CoV-2nsp14-IN-10(CompoundC10)(60-180mg/kg,i.p.,twicedailyfor3days)effectivelyreducesSARS-CoV-2replicationandpathologicaldamageinthelungsofK18-hACE2transgenicmiceinfectedwithSARS-CoV-2,withabroadsafetymargin[1].AnimalModel:Thesix-toeight-week-oldmaleK18-hACE2transgenicmice(18-20g)wereinoculatedintranasallywith5×103focus-formingunitsofSARS-CoV-2nCoV-SH01strain[1].Dosage:60mg/kg,120mg/kg,180mg/kgAdministration:I.p.,twicedailyfor3daysResult:120mg/kgsignificantlyreducedpulmonaryviraltiter.60mg/kgshowedadecreasingtrend,buttheeffectwasnotstatisticallysignificant.Reducedalveolarwallthickening,congestion,andinflammatoryinfiltration.ThepositivesignaloftheSARS-CoV-2nucleocapsidproteinwassignificantlyreduced.REFERENCES[1].LuoM,etal.SARS-CoV-2NSP14inhibitorexhibitspotentantiviralactivityandreversesNSP14-drivenhostmodulation.NatCommun.2025Nov3;16(1):9671.McePdfHeightCaution:Producthasnot