TH10785-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETH10785Cat.No.:HY-147313CASNo.:1002801-51-5分⼦式:C₁₇H₂₁N₃分⼦量:267.37作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3yearsInsolvent-80°C6months-20°C1monthBIOLOGICALACTIVITY⽣物活性TH10785DNA糖化酶1(OGG1)的激活剂。TH10785能与OGG1的苯丙氨酸-319和⽢氨酸-42氨酸相互作⽤，提⾼酶活性，产⽣β,δ裂解酶的酶促功能。TH10785可在分⼦结构上控制氮碱介导的催化活性。TH10785可⽤于与DNA氧化损伤相关的各种疾病和衰⽼的研究。IC50&TargetOGG1(KD=5.5μM)[1]体外研究TH10785(6.25μM,30min)inducesadenovoβ,δ-eliminationinvitro,allowingforAPsitesasnewsubstrates[1].TH10785(10μM,0-2min)allowsOGG1toincreaseDNArepairbyaddressingAPsites[1].TH10785(0-20μM,72h)inducesOGG1β,δ-lyaseactivityshiftscellstowardPNKP1dependence[1].TH10785(2μM)hasaffinitytoOGG1(KD=5.5μM)increasedwhenaddinganAPsiteanalogcontainingdouble-strandedDNA(KD=1.3μM)[1].CellViabilityAssay[1]CellLine:U2OScellsConcentration:0-20μMIncubationTime:72hoursResult:ReducedcombinationwithPNKP1inhibitionforTH10785.WesternBlotAnalysis[1]1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:U2OScellsConcentration:0.65μM;10μMIncubationTime:30min;24hResult:Causedanup-regulationofmembersoftheDDRthroughβ,δ-eliminationincombinationwithPNKP1inhibitionandAPE1-independentdenovoβ,δ-eliminationofAPsitesbyOGG1inthepresenceofTH10785.RT-PCR[1]CellLine:U2OScellsConcentration:10μMIncubationTime:1hResult:Decreasedoxidativedamageinguanine-richregionsofthegenome.Immunofluorescence[1]CellLine:U2OSOGG1-GFPcellsConcentration:1μMIncubationTime:0-2minResult:EcruitedmoreOGG1tolaser-damagedsites.REFERENCES[1].MauriceMichel,etal.Small-moleculeactivationofOGG1increasesoxidativeDNAdamagerepairbygaininganewfunction.Science.2022Jun24;376(6600):1471-1476.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820