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 pp140trk 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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
MAP kinase kinase (MEK)
Product does not compete with ATP.
Reversible: yes
Target IC50: 2 µM in completely blocking the 4-fold increase in MAP kinase activity produced by nerve growth factor in PC12 cells
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
Physical form
A 5 mg/ml solution of PD 98059 (Cat. No. 513000) in anhydrous DMSO.
Reconstitution
Following initial thaw, aliquot and freeze.
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 Citations
Lee, J., et al. 2009. Cell Stem Cell5, 76.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51282614
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 513001-1ML