Background:

PD98059 is a selective and reversible inhibitor of MAPK-activating enzyme, MAPK/ERK kinase (MEK) that inhibits either basal MEK (GST-MEK1) or a partially activated MEK produced by mutation of serine to glutamate at 218 and 222 residues (GST-MEK-2E) with IC50 values of 10uM [1].
PD98059 treatment resulted in distinct changes in cell morphology and density compared to control cells treated with DMSO. PD98059 inhibited proliferation or induced cell death in human leukemic U937 cells. Additionally, PD98059 dose-dependently inhibited the ERK1/2 phosphorylation as well as down-regulated cyclin E/Cdk2 and cyclin D1/Cdk4 levels, resulting in G1 phase arrest and apoptosis induction in U937 cells [2].
参考文献:
[1] Dudley DT1, Pang L, Decker SJ, Bridges AJ, Saltiel AR. A synthetic inhibitor of the mitogen-activated protein kinase cascade. Proc Natl Acad Sci U S A. 1995 Aug 15;92(17):7686-9.
[2] Moon DO1, Park C, Heo MS, Park YM, Choi YH, Kim GY. PD98059 triggers G1 arrest and apoptosis in human leukemic U937 cells through downregulation of Akt signal pathway. Int Immunopharmacol. 2007 Jan;7(1):36-45. Epub 2006 Sep 8.