TH10785-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETH10785Cat.No.:HY-147313CASNo.:1002801-51-5分?式:C??H??N?分?量:267.37作?靶點:Others作?通路:Others儲存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1monthBIOLOGICALACTIVITY?物活性TH10785DNA糖化酶1(OGG1)的激活劑。TH10785能與OGG1的苯丙氨酸-319和?氨酸-42氨酸相互作?，提?酶活性，產(chǎn)?β,δ裂解酶的酶促功能。TH10785可在分?結(jié)構(gòu)上控制氮堿介導的催化活性。TH10785可?于與DNA氧化損傷相關的各種疾病和衰?的研究。IC50&TargetOGG1(KD=5.5μM)[1]體外研究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?邊的抑制劑?師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