AMG-47a

AMG-47a is a potent inhibitor of Lck and T cell proliferation. It exhibits anti-inflammatory activity (ED₅₀ = 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice. In several other in vitro assays, AMG-47 displays subnanomolar inhibition against Lck, and low (<10 nM) inhibition against other hard to inhibit kinases such as KDR and SRC and MAPK α (p38α). In addition, at slightly higher doses but well under 10 µM, AMG-47 effectively inhibits the JNK family of kinases including TYK2 at ~ 1.2 µM.