AX-15836-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAX-15836Cat.No.:HY-101846CASNo.:2035509-96-5分⼦式:C₃₂H₄₀N₈O₅S分⼦量:648.78作⽤靶点:ERK作⽤通路:MAPK/ERKPathway;StemCell/Wnt储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(154.14mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5414mL7.7068mL15.4135mL5mM0.3083mL1.5414mL3.0827mL10mM0.1541mL0.7707mL1.5414mL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(3.85mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(3.85mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.85mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性AX-15836有效，选择性的ERK5抑制剂，IC50值为8nM。IC50&TargetERK58nM(IC50)体外研究AX-15836showsmorethan1,000-foldselectivityforERK5overapanelofover200kinases.ItalsoexhibitsselectivityoverBRD4withaKdof3,600nM.AX15836showssimilarintracellularpotency(4–9nM)acrossallcellstested,includingperipheralbloodmononuclearcells(PBMCs),endothelialcells,andoncogeniccelllines.AX15836wascompletelyineffective(EC50>10μM)tosuppressinflammatorycytokineresponse,suggestingthatitwastheBRDinhibitioncomponentofthecompoundsthatmediatedcytokinereduction.InHUVECandHeLacelltypes,samplestreatedwithAX15836showsveryfewgenestobedifferentiallyexpressed.AX15836couldclearlyinhibittheEGF-stimulated,phosphorylatedformofERK5inHeLacells[1].PROTOCOLCellAssay[1]Forproliferationstudies,cellsaretreatedwitheight-pointserialdilutionseriesofAX-15836(startingconcentrationof15μM)orwithDMSOvehicle(0.25%finalvolume).ForMM.1Scells,compoundwasadded1hbeforeaddingrecombinanthumanIL-6at5nM.After3d,therelativenumberofviablecellswasmeasuredviaquantitationofATPusingCellTiter-Glo2.0reagent.LuminescencewasreadontheSynergy2multimodereader[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•MedComm.04March2022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LinEC,etal.ERK5kinaseactivityisdispensableforcellularimmuneresponseandproliferation.ProcNatlAcadSciUSA.2016Oct18;113(42):11865-11870.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical