Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAX-15836Cat.No.:HY-101846CASNo.:2035509-96-5分?式:C??H??N?O?S分?量:648.78作?靶點:ERK作?通路:MAPK/ERKPathway;StemCell/Wnt儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(154.14mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.5414mL7.7068mL15.4135mL5mM0.3083mL1.5414mL3.0827mL10mM0.1541mL0.7707mL1.5414mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(3.85mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(3.85mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.85mM);ClearsolutionBIOLOGICALACTIVITY?物活性AX-15836有效，選擇性的ERK5抑制劑，IC50值為8nM。IC50&TargetERK58nM(IC50)體外研究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.戶使?本產(chǎn)品發(fā)表的科研?獻?MedComm.04March2022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LinEC,etal.ERK5kinaseactivityisdispensableforcellularimmuneresponseandproliferation.ProcNatlAcadSciUSA.2016Oct18;113(42):11865-11870.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical