KEA1-97-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEKEA1-97Cat.No.:HY-114982CASNo.:2138882-71-8分⼦式:C₁₅H₉Cl₂FN₄分⼦量:335.16作⽤靶点:Caspase;Apoptosis作⽤通路:Apoptosis储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:100mg/mL(298.36mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.9836mL14.9182mL29.8365mL5mM0.5967mL2.9836mL5.9673mL10mM0.2984mL1.4918mL2.9836mL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(protectfromlight)。-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>>90%cornoilSolubility:≥2.5mg/mL(7.46mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性KEA1-97⼀种选择性Thioredoxin-caspase3相互作⽤⼲扰剂(IC50=10μM)。KEA1-97在不响thioredoxin活性的情况下,破坏thioredoxin与caspase3的相互作⽤,激活caspases,诱导细胞apoptosis[1]。IC50&TargetCaspase3Thioredoxin10μM(IC50)10μM(IC50)体外研究KEA1-97(100μM;231MFPcells)impairesthioredoxinpulldownofcaspase3[1].KEA1-97(10μM;48hours;231MFPcells)impaires231MFPserum-freecellproliferation[1].KEA1-97(10μM;0~12hours;231MFPcells)activatescaspase3/7andinducesapoptoticcelldeath[1].KEA1-97(231MFPcells)resistantstosurvivalandproliferationimpairments[1].WesternBlotAnalysis[1]CellLine:231MFPcellsConcentration:100μMIncubationTime:Result:Impairedthioredoxinpulldownofcaspase3.CellProliferationAssay[1]CellLine:231MFPcellsConcentration:10μMIncubationTime:48hResult:Impaired231MFPserum-freecellproliferation.ApoptosisAnalysis[1]CellLine:231MFPcellsConcentration:10μMIncubationTime:0~12hResult:Activatedcaspase3/7andinducedapoptoticcelldeath.体内研究KEA1-97(5mg/kg;i.p.;50days)attenuatestumorxenograftgrowth[1].AnimalModel:Immune-deficientSCIDmiceDosage:5mg/kg2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:I.p.;50daysResult:Attenuatedtumorxenograftgrowth.REFERENCES[1].AndersonKE,etal.Chemoproteomics-EnabledCovalentLigandScreeningRevealsaThioredoxin-Caspase3InteractionDisruptorThatImpairsBreastCancerPathogenicity.ACSChemBiol.2017;12(10):2522-2528.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For