Merck, 444968-5MG, MEK1/2 Inhibitor III, PD0325901

General description
PD-0325901 is a highly effective oral small-molecule inhibitor that targets both mitogen-activated protein kinase kinase 1 (MEK1) and MEK2. It is a selective, non-ATP-competitiveinhibitor of these two MEK isoforms. This cell-permeable benzamide compound is a selective non-competitive inhibitor of MAPKK/MKK, effectively blocking cellular Erk1/2 phosphorylation. In serum-starved HeLa cells, it achieves over 90% inhibition after serum stimulation, while in C26 cells, it reduces phosphorylation by 50% at inhibitor concentrations of 25 nM and 0.33 nM, respectively. The compound exhibits minimal to no effect on Erk1/2 activity ora panel of 66 other kinases, even at concentrations as high as 10 µM in cell-free kinase assays. PD-0325901 has demonstrated oral bioavailability inmice, successfully suppressing both tumor growth and Erk phosphorylation in BRAF(V600E)-expressing SKMEL28 cell-derived tumors in vivo.
Application
PD 0325901 has been used as:·

a supplement in induced pluripotent stem cells (iPSC) medium to culture MEF feeder layers with reprogrammed cells
mitogen-activated protein kinase kinase1/2 (MEK1/2) inhibitor to treat the cells to identify G1 phase cells that had crossed the restriction point in the cell cycle
Mek1/2 inhibitor to block the Ras-Erk1/2 signaling pathwayto investigate the role of fibroblast growth factor (Fgf) signaling in the specification of endoderm progenitors during embryonic development

Packaging
Packaged under inert gas
Physical form
A 50 mM (5 mg/207 µl) solution of MEK1/2 Inhibitor III, PD0325901 (Cat. No. 444966 ) in DMSO.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)