TMBIM6-antagonist-1-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemETMBIM6antagonist-1Cat.No.:HY-137175CASNo.:123134-61-2分⼦式:C₁₅H₁₂N₂O₃分⼦量:268.27作⽤靶点:mTOR作⽤通路:PI3K/Akt/mTOR储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCOA.溶解性数据体外实验DMSO:50mg/mL(186.38mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.7276mL18.6379mL37.2759mL5mM0.7455mL3.7276mL7.4552mL10mM0.3728mL1.8638mL3.7276mL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；该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。BIOLOGICALACTIVITY⽣物活性TMBIM6antagonist-1⼀个有潜⼒的TMBIM6拮抗剂，抑制TMBIM6与mTORC2结合，降低mTORC2活性，调节TMBIM6释放Ca2+。体外研究TMBIM6antagonist-1(BIA,0.5-10μM,3days)significantlyanddose-dependentlyinhibitscellviabilityinHT1080,MCF7,MDA-MB-2341andSKBR3cells,withIC50valuesof1.7ꢀ±ꢀ0.1ꢀμMforHT1080,2.6ꢀ±ꢀ0.4ꢀμMforMCFcells,2.6ꢀ±ꢀ0.5ꢀμMforMDA-MB-231cells,and2.4ꢀ±ꢀ0.4ꢀμMforSKBR3cells,respectively[1].TMBIM6antagonist-1(BIA,10μM)treatmentdecreasescellmigrationinHT1080,MCF7,MDA-MB-231,andSKBR3cells,notTMBIM6KOHT1080cells[1].1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemECellViabilityAssay[1]CellLine:HT1080,MCF7,MDA-MB-2341andSKBR3cells.Concentration:0.5-10μM.IncubationTime:3days.Result:Inhibitedcellviability.WesternBlotAnalysis[1]CellLine:WTandTMBIM6KOHT1080cells.Concentration:0,2,5μM.IncubationTime:Result:DownregulatedtheproteinlevelsofAKT-pS473.体内研究TMBIM6antagonist-1(1ꢀmg/kg,IP5daysperweekduring25days)significantlyimpairescell-driventumorgrowth[1].AnimalModel:Six-toeight-weekBklNbt:BALB/c/nu/nuoldmice(HT1080andMDA-MB-231cells)[1].Dosage:1ꢀmg/kg.Administration:IP5daysperweekduring25days.Result:Impairedcell-driventumorgrowth.REFERENCES[1].Hyun-KyoungKim,etal.TMBIM6/BI-1contributestocancerprogressionthroughassemblywithmTORC2andAKTactivation.NatCommun.2020Aug11;11(1):4012.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: