Biochem/physiol Actions

Reversible: yes

Product does not compete with ATP.

Target IC₅₀: 2 µM in completely blocking the 4-fold increase in MAP kinase activity produced by nerve growth factor in PC12 cells

Primary TargetMAP kinase kinase (MEK)

Cell permeable: yes

General description

Selective and cell-permeable inhibitor of MAP kinase kinase (MEK) that acts by inhibiting the activation of MAP kinase and subsequent phosphorylation of MAP kinase substrates. Pretreatment of PC-12 cells with PD 98059 completely blocks the 4-fold increase of MAP kinase activity produced by nerve growth factor (NGF; IC₅₀ = 2 µM); however, it has no effect on NGF-dependent tyrosine phosphorylation of the pp140^trk receptor or its substrate Shc and does not block NGF-dependent activation of PI 3-kinase. Inhibits cell growth and reverses the phenotype of ras-transformed BALB 3T3 mouse fibroblasts and rat kidney cells.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Kültz, D., et al. 1998. J. Biol. Chem.273, 13645.Dudley, D.T., et al. 1995. Proc. Natl. Acad. Sci. USA92, 7686.Langlois, W.J., et al. 1995. J. Biol. Chem.270, 25320.Pang, L., et al. 1995. J. Biol. Chem.270, 13585.Waters, S.B., et al. 1995. J. Biol. Chem.270, 20883.Selected CitationsLee, J., et al. 2009. Cell Stem Cell5, 76.

Packaging

Packaged under inert gas

1 ml in Glass bottle

Physical form

A 5 mg/ml solution of PD 98059 (Cat. No. 513000) in anhydrous DMSO.

Reconstitution

Following initial thaw, aliquot and freeze.

Warning

Toxicity: Irritant (B)