LJI308-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELJI308Cat.No.:HY-19713CASNo.:1627709-94-7分⼦式:C₂₁H₁₈F₂N₂O₂分⼦量:368.38作⽤靶点:RibosomalS6Kinase(RSK)作⽤通路:MAPK/ERKPathway储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(67.86mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7146mL13.5729mL27.1459mL5mM0.5429mL2.7146mL5.4292mL10mM0.2715mL1.3573mL2.7146mL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>>90%cornoilSolubility:≥2.5mg/mL(6.79mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性LJI308⼀种有效的泛RSK抑制剂，对RSK1、RSK2和RSK3的IC50分别为6nM、4nM和13nM。LJI308抑制辐照、EGF处理和表达KRAS突变的细胞中RSK(T359/S363)和YB-1(S102)的磷酸化。体外研究LJI308inhibitsS6K1withanIC50of0.8μM[1].LJI308inhibitsYB-1phosphorylationinCRCcellsatconcentrationsof5to25μM.Inadosekineticsexperiment,LJI308,startingat2.5μM,inhibitsYB-1phosphorylationintheKRASmutatedTNBCcelllineMDA-MB-231byapproximately86%.LJI308effectivelyblocksRSKandYB-1phosphorylationafterEGFstimulationandafterirradiationinKRASwild-typeHBL-100cells[2].LJI308(1-10μM;96hours)decreasescellviabilitybyupto90%[3].CellViabilityAssay[3]CellLine:HTRY-LTcelllinesConcentration:1-10μMIncubationTime:96hoursResult:Decreasedcellviabilitybyupto90%.户使⽤本产品发表的科研⽂献•Circulation.2022Nov30.•JInvestDermatol.2020Sep9;S0022-202X(20)32055-8.•Oncotarget.2017Jun6;8(23):37633-37645.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].AronchikI,etal.Novelpotentandselectiveinhibitorsofp90ribosomalS6kinaserevealtheheterogeneityofRSKfunctioninMAPK-drivencancers.MolCancerRes.2014May;12(5):803-12.[2].LettauK,etal.SimultaneousTargetingofRSKandAKTEfficientlyInhibitsYB-1-MediatedRepairofIonizingRadiation-InducedDNADouble-StrandBreaksinBreastCancerCells.IntJRadiatOncolBiolPhys.2021;109(2):567-580.[3].JainR,etal.DiscoveryofPotentandSelectiveRSKInhibitorsasBiologicalProbes.JMedChem.2015Sep10;58(17):6766-83.[4].DaviesAH,etal.InhibitionofRSKwiththenovelsmall-moleculeinhibitorLJI308overcomeschemoresistancebyeliminatingcancerstemcells.Oncotarget.2015;6(24):20570-20577.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplic