An orally bioavailable and potent inhibitor of MEK1/2 inhibitor (IC50 = 8 nM); selective for MEK1/2 over ERK, c-Src, PI3Kγ, and cyclin-dependent kinases (IC50s = >1 μM); reduces ERK1/2 phosphorylation and inhibits growth of HL-60 cells in vitro; reduces ERK1/2 phosphorylation and MMP-1 expression in a dose-dependent manner in a rabbit model of osteoarthritis when administered at doses ranging from 10-30 mg/kg; reduces ERK1/2 activity in the lumbar spinal cord and blocks static allodynia in rat models of streptozotocin- and chronic constriction injury-induced neuropathic pain,