TA-02-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETA-02Cat.No.:HY-100115CASNo.:1784751-19-4分⼦式:C₂₀H₁₃F₂N₃分⼦量:333.33作⽤靶点:p38MAPK;Autophagy作⽤通路:MAPK/ERKPathway;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(75.00mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0000mL15.0002mL30.0003mL5mM0.6000mL3.0000mL6.0001mL10mM0.3000mL1.5000mL3.0000mL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(7.50mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.50mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性TA-02SB203580(HY-10256)的⼀个类似物，p38MAPK的抑制剂，其IC50值为20nM。TA-02可抑制TGFBR-2。TA-02和SB203580、SB202190(HY-10295)具有相似的⼼活性。体外研究TA-02(5μM)inhibitsthephosphorylationofproteinsdownstreamofp38αMAPKsuchasMAPKAPK2andHSP27duringcardiogenesis.TA-02at5μMconcentrationinducescardiogenesis,butalsoincreasesATF-2phosphorylationandMEF2Cõexpressionincontrasttowhatwouldbeexpectedwithamechanismdependentonp38αMAPKinhibition[1].TA-02inducesT/BrachyurywhereasSB203580additionincreasedMESP1andT/Brachyurytranscripts[1].TA-02significantlyinduceshighNKX2-5expressionwhenappliedbetweendays0-8[1].TA-02isfoundtoinhibitmultipletargetswithsimilarpotencytop38αMAPK,suchasp38α,p38β,JNK3,JNK2,CIT,CK1ε,DMPK2,JNK1,DDR1CK1δ,MEK5,andERBB2[1].TA-02andSB203580reducethenuclearTCF/LEF-1driventranscriptionofluciferasesimilartoDKK-1[1].TA-02(5nM-5μM)inhibitsp38andincreasestheanti-inflammationeffectsofBDNFoninflammationinvitro[2].WesternBlotAnalysis[2]CellLine:ThenervecelllineAGE1.HN.Concentration:5nM-5μM.IncubationTime:44h(100ng/mlLPSfor4hat37°C).Result:Suppressedp-38proteinexpression,reducedIL-1β,IL-6,IL-18andTNF-αlevelsandinhibitediNOSandCOX-2levelsinaninvitromodelofSCIbyBDNFoverexpression,comparedwiththeBDNFoverexpressiongroup.户使⽤本产品发表的科研⽂献•ExpTherMed.2019Mar;17(3):1688-1696.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LacoF,etal.CardiomyocytedifferentiationofpluripotentstemcellswithSB203580analoguescorrelateswithWntpathwayCK1inhibitionindependentofp38MAPKsignaling.JMolCellCardiol.2015Mar;80:56-70.[2].JiedongLiang,etal.TheactivationofBDNFreducedinflammationinaspinalcordinjurymodelbyTrkB/p38MAPKsignaling.ExpTher2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEMed.2019Mar;17(3):1688-1696.McePdfHeightCaution:Producthasnotbeenfullyvalidated