LJH685-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELJH685Cat.No.:HY-19712CASNo.:1627710-50-2分⼦式:C₂₂H₂₁F₂N₃O分⼦量:381.42作⽤靶点:RibosomalS6Kinase(RSK);Apoptosis作⽤通路:MAPK/ERKPathway;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥31mg/mL(81.28mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.6218mL13.1089mL26.2178mL5mM0.5244mL2.6218mL5.2436mL10mM0.2622mL1.3109mL2.6218mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥1mg/mL(2.62mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1mg/mL(2.62mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1mg/mL(2.62mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性LJH685⼀种有效的选择性，ATP-竞争性的RSK抑制剂,抑制RSK1/2/3⽣物活性,IC50为6、5、4nM。IC50&TargetIC50:6nM(RSK1),5nM(RSK1),4nM(RSK1)[1]体外研究LJH685(0.01-100μM;72hours)efficientlyinhibitsthegrowthofMDA-MB-231andH358cellsinsoftagarwithEC50sof0.73and0.79μM,respectively[1].LJH685(0.1-10μM;4hours)efficientlyreducesphosphorylationofYB1atsubmicromolarconcentrationsandcausesnearlycompleteinhibitionathigherconcentrations[1].CellProliferationAssay[1]CellLine:MDA-MB-231,H358cellsConcentration:0.01,0.1,1,10,100μMIncubationTime:72hoursResult:ThegrowthinsoftagarwasefficientlyinhibitedwithEC50valuesof0.73and0.79μMinMDA-MB-231andH358,respectively.WesternBlotAnalysis[1]CellLine:MDA-MB-231,H358cellsConcentration:0.1,0.3,1,3,10μMIncubationTime:4hoursResult:EfficientlyreducedphosphorylationofYB1atsubmicromolarconcentrationsandcausednearlycompleteinhibitionathigherconcentrations.户使⽤本产品发表的科研⽂献•CellDeathDiffer.2022Jan13.•JInvestDermatol.2020Sep9;S0022-202X(20)32055-8.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].AronchikI,etal.Novelpotentandselectiveinhibitorsofp90ribosomalS6kinaserevealtheheterogeneityofRSKfunctioninMAPK-drivencancers.MolCancerRes.2014May;12(5):803-12.[2].DaviesAH,etal.InhibitionofRSKwiththenovelsmall-moleculeinhibitorLJI308overcomeschemoresistancebyeliminatingcancerstemcells.Oncotarget.2015Aug21;6(24):20570-7.[3].JainR,etal.DiscoveryofPotentandSelectiveRSKInhibitorsasBiologicalProbes.JMedChem.2015Sep10;58(17):6766-83.[4].My-MyHuynh,etal.RSK2:apromisingtherapeutictargetforthetreatmentoftriple-negativebreastcancer.ExpertOpinTherTargets.2020Jan;24(1):1-5.McePdfHeightCaution:Producthasnotbeenfullyvalidat