NecroIr2-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENecroIr2Cat.No.:HY-148366分⼦式:C₄₆H₃₀ClIrN₆O₂分⼦量:926.44作⽤靶点:MixedLineageKinase;RIPkinase;CDK作⽤通路:MAPK/ERKPathway;Apoptosis;CellCycle/DNADamage储存⽅式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性数据体外实验DMSO:50mg/mL(53.97mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.0794mL5.3970mL10.7940mL5mM0.2159mL1.0794mL2.1588mL10mM0.1079mL0.5397mL1.0794mL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(sealedstorage,awayfrommoistureandlight)。-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。BIOLOGICALACTIVITY⽣物活性NecroIr2⼀种铱(III)复合物，(Cisplatin,HY-17394)耐药肺癌细胞(A549R)的坏死诱导剂。NecroIr2选择性积累在线粒体中，导致氧化应激和线粒体膜电位(MMP)的损失。NecroIr2能够激活受体相互作⽤的丝氨酸苏氨酸激酶3(RIPK3)和混合谱系激酶结构域样假激酶(MLKL)，调节CDK4表达。IC50&TargetCDK4RIPK3RIPK1体外研究NecroIr2(2μM;1-2d)exertssubcellulardistributionover90%accumulatedinmitochondriainnon-labelledA549RandCFSElabelledL02cells[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemENecroIr2(1.5μMand3μM;24h)resultsROSgenerationincreasingandlossofmitochondrialmembranepotential[1].NecroIr2(1.5μMand3μM;24h)activatesnecroptosisproteins,increasesthephosphorylationofRIPK1andRIPK3[1].NecroIr2(0.75μMand1.5μM;24h)inducesnecroptosisbyarrestingcellcycleatG0/G1[1].NecroIr2(0.375-1.5μM;24h)inhibitsA549Rcellsproliferation[1].WesternBlotAnalysis[1]CellLine:A549RcellsConcentration:1.5μMand3μMIncubationTime:24hoursResult:Increasedphospho-RIPK1(p-PIPK1),totalRIPK3,andphospho-RIPK3(p-PIPK3)level.CellCycleAnalysis[1]CellLine:A549RcellsConcentration:0μM,0.75μMand1.5μMIncubationTime:24hoursResult:ArrestedcellcycleatG0/G1phaseinadose-dependentmanner.CellProliferationAssay[1]CellLine:A549RcellsConcentration:0μM,0.375μM,0.75μMand1.5μMIncubationTime:24hoursResult:Inhibitscellproliferationinadose-dependentmanner.REFERENCES[1].GuanR,etal.Necroptosis-inducingiridium(III)complexesasregulatorsofcyclin-dependentkinases[J].InorganicChemistryFrontiers,2021,8(7):1788-1794.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc