Nrf2-IN-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENrf2-IN-1Cat.No.:HY-101025CASNo.:1610022-76-8分⼦式:C₂₁H₂₂ClN₃O₂分⼦量:383.87作⽤靶点:Keap1-Nrf2作⽤通路:NF-κB储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:260mg/mL(677.31mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.6050mL13.0252mL26.0505mL5mM0.5210mL2.6050mL5.2101mL10mM0.2605mL1.3025mL2.6050mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.17mg/mL(5.65mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.17mg/mL(5.65mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.17mg/mL(5.65mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Nrf2-IN-1Nrf2的抑制剂，被⽤于急性髓性⽩⾎病(AML)药物研究[1]。IC50&TargetNrf2[1]体外研究Nrf2-IN-1(Compound4f)(10μM)inhibitsNrf2activation[1].Nrf2-IN-1(1-20μM;48hours)inhibitsgrowthofthethreeAMLcell[1].Nrf2-IN-1(5-10μM;48hours)inducesapoptosisofthreeAMLcellsinvitro[1].Nrf2-IN-1inducesapoptoticsignalinginvolvingBcl-2andBax[1].CellViabilityAssay[1]CellLine:THP-1cells,HL-60cells,U937cellsConcentration:1μM,5μM,10μM,20μMIncubationTime:48hoursResult:InhibitedgrowthofthethreeAMLcelltypesat5μM,10μMor20μMfor48hours.ApoptosisAnalysis[1]CellLine:THP-1cells,HL-60cells,U937cellsConcentration:5μM,10μMIncubationTime:48hoursResult:InducedapoptosisinAMLcellsinvitro.WesternBlotAnalysis[1]CellLine:THP-1cells,HL-60cells,U937cellsConcentration:5μM,10μMIncubationTime:48hoursResult:Triggeredcaspase-dependentapoptoticsignalinginAMLcells.体内研究Nrf2-IN-1inhibitstumorgrowthviaapoptosisinchickeneggs[1].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE户使⽤本产品发表的科研⽂献•CellsTissuesOrgans.July08,2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZhangJ,etal.DiscoveryofanovelNrf2inhibitorthatinducesapoptosisofhumanacutemyeloidleukemiacells.Oncotarget.2017Jan31;8(5):7625-7636.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.F