A JAK Inhibitor
Tyrphostin AG-490 (AG-490) is synthetic tyrphostin derivated from benzylidine malononitrile. At relatively low concentrations, AG-490 was found to be a highly efficient tyrosine kinase inhibitor for hyperactive forms of Jun kinase 2, 3 and 5 (Jak 2,3, and 5).
While many kinase inhibitors are often promiscuous in the enzymes they target, AG-490 is unique in that it does not inhibit other lymphocytic tyrosine kinases such as Lck, Lyn, Btk, Syk, Src, Jak1, Zap70 or Tyk2. AG-490 has also been shown to inhibit cytokine-induced activation of JAK2 in eosinophils stimulated with granulocyte-macrophage and in vascular smooth muscle cells and cardiac myocytes activated by angiotensin
Some studies have demonstrated that AG-490 efficiently blocks STAT3 activation in mycosis fungoides-derived T cell lymphoma cells and induces apoptosis in myeloma cells.
Protein Kinase Inhibitors and Activators; JAK Inhibitor.