Description
TyrphostinAG490inhibitsJAK2andexhibitsanti-diabetic,anti-atherosclerotic,immunosuppressive,andanticanceractivities.TyrphostinAG490inhibitsjointinflammationinvivobysuppressingactivationofSTAT3,productionofTNF-αandRANKL,anddifferentiationofosteoclasts.TyrphostinAG490alsoinducesprogrammedcelldeathandinhibitsinvasionandadhesionofleukemiacells.Inanimalmodelsofatherosclerosis,tyrphostinAG490decreasesactivityandexpressionofNoxandlevelsofCD68,decreasingtheformationofatheroscleroticlesions.Additionally,tyrphostinAG490increasesexpressionofPPARγanddecreasesbloodglucoselevelsinvivo,preventingtheonsetofautoimmunetype1diabetes.ThiscompoundalsoinhibitsexpressionofMCP-1,IFNγ,andMHCclassII,decreasesinfiltrationofTcellsandmacrophages,andsuppressesdepositionofIgGinanimalmodelsoflupusnephritis.TyrphostinAG490mayalsoinhibitEGFR.
References
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