CAY10561

The extracellular signal-regulated kinase (ERK) signal transduction pathway regulates a diverse array of cellular processes. These processes include cell survival, proliferation, motility, and differentiation and are constitutively activated in cancers involving lung, colon, pancreas, kidney, and ovary.¹ CAY10561 is a potent, ATP-competitive inhibitor of ERK2 (K_i = 2 nM).² This compound is highly selective for ERK2 compared to other kinases such as PKA (K_i = 0.39 μM) and JNK3 (K_i = 4 μM).² CAY10561 inhibits proliferation of COLO 205 cells with an IC₅₀ value of 0.54 μM.²

1. Junttila, M.R., Li, S.P., and Westermarck, J. Phosphatase-mediated crosstalk between MAPK signaling pathways in the regulation of cell survival FASEB J. 22,1-12(2008).
2. Aronov, A.M., Baker, C., Bemis, G.W., et al. Flipped out: Structure-guided of selective pyrazolylpyrrole ERK inhibitors J. Med. Chem. 50,1280-1287(2007).