Overview
- Wang, L.H. et al. (1999) J. Immunol. 162, 3897.
Alomone Labs Tyrphostin AG 490 inhibits the proliferation of Jurkat cells.Cells were treated with different concentrations of Tyrphostin AG 490 (#T-700) for 4 days. Cell survival was measured after 4 days using the XTT method, calculated as a relative percentage of the control without Tyrphostin AG 490 and plotted against drug concentrations.
Tyrphostin AG-490 (AG-490) is synthetic tyrphostin derived from benzylidine malononitrile.1 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. 2-6 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 II. 7-9
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.10-11
