PD 184161

The mitogen-activated protein (MAP) kinase intracellular signaling pathways are involved in the regulation of various cellular functions.¹ One of these pathways, the Raf/MEK/ERK pathway, plays a major role in the regulation of cellular growth, differentiation, and proliferation. The modulation of this cascade has been studied as a useful approach to treating proliferative disorders such as cancer.^2,3 PD 184161 is a potent and selective inhibitor of MEK1/2 with an IC₅₀ value that ranges from 10-100 nM. ⁴ More effective at inhibiting phosphorylation of ERK1/2 than the selective MEK inhibitors, PD 098059 and U0126, PD 184161 is useful both in vitro and in vivo for studying the pharmacological role of the Raf/MEK/ERK pathway.⁴ PD 184161 is structurally related to clinically-studied MEK inhibitors PD184352 (CI-1040) and PD 325901 and has been shown to inhibit cell proliferation, induce apoptosis, and possess antitumor activity in MEK-dependent cancers.⁴

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1. Cowan, K.J., and Storey, K.B. Mitogen-activated protein kinases: New signaling pathways functioning in cellular responses to environmental stress. J. Exp. Biol. 206(Pt 7), 1107-1115 (2003).

2. Dhillon, A.S., Hagan, S., Rath, S., et al. MAP kinase signalling pathways in cancer. Oncogene 26, 3279-3290 (2007).

3. VanScyoc, W.S., Holdgate, G.A., Sullivan, J.E., et al. Enzyme kinetics and binding studies on inhibitors of MEK protein kinase. Biochemistry 47, 5017-5027 (2008).

4. Klein, P.J., Schmidt, C.M., Wiesenauer, C.A., et al. The effects of a novel MEK inhibitor PD184161 on MEK-ERK signaling and growth in human liver cancer. Neoplasia 8(1), 1-8 (2006).