PD184161 is a potent, orally-active MEK1/2 inhibitor with IC50 of 10-100 nM.
PD184161inhibits HCC cell proliferation and induced apoptosis at concentrations of > or = 1.0 uM, significantly suppresses tumor engraftment and initial growth in tumor xenografts.
PD184161 also blocks AngII-driven HIF-1α protein in vascular smooth muscle cells, increases HIF-1α binding to von Hippel-Lindau tumor suppressor protein, blocks mitochondrial ROS production and cellular ATP levels.
