PD 198306

PD 198306

CAT N°: 23966
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From 100.00 85.00

PD 198306 is an orally bioavailable and potent inhibitor of MAPK kinase 1/2 (MEK1/2; IC50 = 8 nM).{38577} It is selective for MEK1/2 over ERK, c-Src, PI3K?, and cyclin-dependent kinases (IC50s = >1 ?M). PD 198306 (3-100 ?M) reduces ERK1/2 phosphorylation and inhibits growth of HL-60 cells in vitro.{38578} In vivo, PD 198306 (10-30 mg/kg) reduces ERK1/2 phosphorylation and matrix metalloproteinase-1 (MMP-1) expression in a dose-dependent manner in a rabbit model of osteoarthritis.{38577} It also reduces ERK1/2 activity in the lumbar spinal cord and blocks static allodynia in rat models of neuropathic pain induced by streptozotocin (Item No. 13104) or chronic constriction injury.{38579}

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