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 (Ki = 2 nM).2 This compound is highly selective for ERK2 compared to other kinases such as PKA (Ki = 0.39 µM) and JNK3 (Ki = 4 µM).2 CAY10561 inhibits proliferation of Colo205 cells with an IC50 value of 0.54 µM.2
1
Junttila, M.R., Li, S., and Westermarck, J. Phosphatase-mediated crosstalk between MAPK signaling pathways in the regulation of cell survival. FASEB J221-12(2008).
2
Aronov, A.M., Baker, C., Bemis, G.W., et al. Flipped out: Structure-guided of selective pyrazolylpyrrole ERK inhibitors. J Med Chem501280-1287(2007).
Junttila, M.R., Li, S., and Westermarck, J. Phosphatase-mediated crosstalk between MAPK signaling pathways in the regulation of cell survival. FASEB J221-12(2008).
Aronov, A.M., Baker, C., Bemis, G.W., et al. Flipped out: Structure-guided of selective pyrazolylpyrrole ERK inhibitors. J Med Chem501280-1287(2007).
CAY10561 is available in the following screening
library: