Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENecroIr2Cat.No.:HY-148366分?式:C??H??ClIrN?O?分?量:926.44作?靶點:MixedLineageKinase;RIPkinase;CDK作?通路:MAPK/ERKPathway;Apoptosis;CellCycle/DNADamage儲存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(53.97mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.0794mL5.3970mL10.7940mL5mM0.2159mL1.0794mL2.1588mL10mM0.1079mL0.5397mL1.0794mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoistureandlight)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。BIOLOGICALACTIVITY?物活性NecroIr2?種銥(III)復合物，(Cisplatin,HY-17394)耐藥肺癌細胞(A549R)的壞死誘導劑。NecroIr2選擇性積累在線粒體中，導致氧化應激和線粒體膜電位(MMP)的損失。NecroIr2能夠激活受體相互作?的絲氨酸蘇氨酸激酶3(RIPK3)和混合譜系激酶結(jié)構(gòu)域樣假激酶(MLKL)，調(diào)節(jié)CDK4表達。IC50&TargetCDK4RIPK3RIPK1體外研究NecroIr2(2μM;1-2d)exertssubcellulardistributionover90%accumulatedinmitochondriainnon-labelledA549RandCFSElabelledL02cells[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師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