The extracellular regulated kinases 1 and 2 (ERK1/2) are functionally redundant kinases activated by a variety of growth factors and mitogens.{17806} FR180204 is a potent cell-permeable inhibitor of ERK1 and ERK2 (Ki = 310 and 140 nM, respectively).{25542} It is much less effective against p38α (IC50 = 10 µM) and does not inhibit a range of other serine/threonine or tyrosine kinases.{25542} FR180204 blocks ERK-mediated signaling from TGF-β to AP-1 (IC50 = 3.1 μM).{25542} It attenuates delayed-type hypersensitivity in collagen-immunized mice and ameliorates collagen-induced arthritis in mice.{25543}
产品描述
A potent cell-permeable inhibitor of ERK1 and ERK2 (Ki = 310 and 140 nM, respectively); much less effective against p38α (IC50 = 10 µM) and does not inhibit a range of other serine/threonine or tyrosine kinases; blocks ERK-mediated signaling from TGF-β to AP-1 (IC50 = 3.1 μM)
