9-ING-41-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE9-ING-41Cat.No.:HY-113914CASNo.:1034895-42-5分⼦式:C₂₂H₁₃FN₂O₅分⼦量:404.35作⽤靶点:GSK-3;Apoptosis;Autophagy作⽤通路:PI3K/Akt/mTOR;StemCell/Wnt;Apoptosis;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(123.66mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4731mL12.3655mL24.7310mL5mM0.4946mL2.4731mL4.9462mL10mM0.2473mL1.2366mL2.4731mL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:2.5mg/mL(6.18mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性9-ING-41⼀种于马来酰亚胺的ATP竞争性和选择性的糖原合酶激酶-3β(GSK-3β)抑制剂，IC50为0.71μM。9-ING-41显著导致癌细胞的细胞周期停滞，⾃噬和凋亡。9-ING-41具有抗癌活性，并具有增强化疗药物抗肿瘤作⽤的潜⼒。IC50&TargetGSK-3β0.71μM(IC50)体外研究9-ING-41(2,4μM;48hours)decreasesneuroblastomacellviabilityinducesapoptosis[2].9-ING-41(1,2μM;24hours)isapotentcellcycle-blockingagentforlymphomacells[2].9-ING-41(10ꢀμM;for72ꢀhours)increasestheexpressionofLC3,anautophagymarker[3].9-ING-41(compound26;5μM;for6,12,24,36h)resultsinapronounceddecreaseinNFκB-mediatedexpressionofXIAP,themostpotentantiapoptoticprotein,leadingtosubsequentapoptosisinBXPC3pancreaticcancercells[1].9-ING-41(0.5,1.0,1.5,2.0μM)inhibitstheproliferationrateofallTCLandMCLlineswithconcentrationsaslowas1.0mM[2].9-ING-41(10ꢀμM;for72ꢀhours)causescellcycleblockageatG2/Mafter24ꢀhours.9-ING-41treatmentinducesapoptoticcelldeathinbladdercancercells[3].9-ING-41(25ꢀμM;for96ꢀhours)significantlydecreasesexpressionofCdk1andCyclinB1proteinsandleadstoadecreasedexpressionofantiapoptoticmolecules,Bcl-2andXIAP[3].9-ING-41(0.1-1µM)inhibitsGSK-3leadingtoadecreasedexpressionoftheNF-κBtargetXIAPandsignificantapoptosisinneuroblastomacellsasshownbyPARPcleavage,anapoptosismarker[4].CellViabilityAssay[2]CellLine:TCLandMCLlinesConcentration:2,4μMIncubationTime:48hoursResult:Inducedapoptosis.CellCycleAnalysis[2]CellLine:Lymphomacells(Jeko,Mino,andOCI-Lycelllines)Concentration:1,2μMIncubationTime:24hoursResult:LedtocellcyclearrestinG2/M.CellAutophagyAssay[3]2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:T24cancercellsConcentration:25ꢀμMIncubationTime:24ꢀhoursResult:Showedextensivevacuolationandformationofautophagosomelikestructuresinthecytoplasm.ShowedanincreasedexpressionofLC3,anautophagymarker.WesternBlotAnalysis[4]CellLine:SK-N-DZandSK-N-BEneuroblastomacellsConcentration:0.1,1µMIncubationTime:48hoursResult:InhibitedGSK-3leadingtoadecreasedexpressionoftheNF-κBtargetXIAP.体内研究9-ING-41(40mg/kg/everyotherday;for17days)hassingle-agentantitumoractivityinamousemodelofMCL[2].AnimalModel:NSG(NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ)mice[2]Dosage:40mg/kgAdministration:Everyotherday;for17daysResult:Hadsingle-agentantitumoractivityinamousemodelofMCL.REFERENCES[1].UgolkovAV,etal.9-ING-41,asmall-moleculeglycogensynthasekinase-3inhibitor,isactiveinneuroblastoma.AnticancerDrugs.2018Sep;29(8):717-724.[2].WuX,etal.Targetingglycogensynthasekinase3fortherapeuticbenefitinlymphoma.Blood.2019Jul25;134(4):363-373.[3].IrinaNGaisina,etal.Fromanaturalproductleadtotheidentificationofpotentandselectivebenzofuran-3-yl-(indol-3-yl)maleimidesasglycogensynthasekinase3betainhibitorsthatsuppressproliferationandsurvivalofpancreaticcancercells.JMe[4].HirooKuroki,etal.9-ING-41,asmallmoleculeinhibitorofGSK-3beta,potentiatestheeffectsofanticancertherapeuticsinbladdercancer.SciRep.2019Dec27;9(1):19977