MIND4-17-DataSheet-生命科學試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMIND4-17Cat.No.:HY-121523CASNo.:345989-24-4分?式:C??H??N?O?S分?量:405.43作?靶點:Keap1-Nrf2作?通路:NF-κB儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性MIND4-17?種有效的NRF2激活劑，可共價修飾Keap1的C151殘。MIND4-17破壞Keap1-Nrf2結(jié)合，導(dǎo)致Nrf2蛋?穩(wěn)定和核易位。MIND4-17具有強?的抗氧化活性。體外研究MIND4-17(0.1-2μM;24hr)significantlyandconcentration-dependentlyincreasestheexpressionofthecanonicalAREgenesNqo1,Hmox1,Srx1,andtoalesserdegreeGclc[1].MIND4-17(0.1-2μM;24hr)showsaconcentration-dependentinductionofNQO1andGCLMproteinsinbothWTandHDmutantST14Acells[1].MIN4-17(0.1-10μM)reducesROSlevelsandnitrogenintermediatesproductioninmicroglia[1].RT-PCR[1]CellLine:RatcorticostriatalneuronalConcentration:1μM,5μMIncubationTime:4hours,16hoursResult:Significantlyandconcentration-dependentlyincreasedtheexpressionofthecanonicalAREgenesNqo1,Hmox1,Srx1,andtoalesserdegreeGclc.WesternBlotAnalysis[1]CellLine:Wild-type(WT)andHuntington'sdisease(HD)mutantST14AcellsConcentration:0.1μM,0.2μM,0.5μM,0.7μM,1μM,1.5μM,2μM1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIncubationTime:24hoursResult:Showedaconcentration-dependentinductionofNQO1andGCLMproteins.體內(nèi)研究eintravitrealinjection;once)activatesNrf2signalingandattenuatesretinaldysfunctionbylightAnimalModel:BALB/cmicebearingwhitefluorescentlightexposure[2]Dosage:2mg/kgAdministration:Intravitrealinjection;onceResult:ActivatedNrf2signalingandattenuatedretinaldysfunctionbylightdamageinmice.REFERENCES[1].LuisaQuinti,etal.SIRT2-andNRF2-TargetingThiazole-ContainingCompoundwithTherapeuticActivityinHuntington'sDiseaseModels.CellChemBiol.2016Jul21;23(7):849-861.[2].NanChen,etal.TheNrf2activatorMIND4-17protectsretinalganglioncellsfromhighglucose-inducedoxidativeinjury.JCellPhysiol.2020Oct;235(10):7204-7213.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Te