Biochem/physiol Actions

Reversible: yes

Product does not compete with ATP.

Primary TargetMAP kinase kinase (MEK)

Cell permeable: yes

Target IC₅₀: 2 µM against NGF-induced increase in MAP kinase activity

General description

Selective, reversible, 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 in MAP kinase activity produced by nerve growth factor (NGF; IC₅₀ = 2 µM); however, it has no effect on NGF-dependent tyrosine phosphorylation of the p140^trk receptor or its substrate Shc and does not block NGF-dependent activation of PI 3-kinase. Blocks LPS-induced activation of TNF-α gene expression. Inhibits cell growth and reverses the phenotype of ras-transformed BALB3T3 mouse fibroblasts and rat kidney cells. A 5 mg/ml solution of PD 98059 (Cat. No. 513001) in anhydrous DMSO is also available.

Selective, reversible, 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 (noncompetitive with respect to ATP). 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

Means, T.K., et al. 2000. J. Leukoc. Biol. 67, 885.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.

Packaging

5 mg in Glass bottle

10, 25 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 4 months at -20°C.

Warning

Toxicity: Standard Handling (A)