产品简称

PD 98059, CAS 167869-21-8, is a cell-permeable, selective & reversible inhibitor of MAP Kinase Kinase (MEK). Inhibits MAP Kinase activation and subsequent phosphorylation of MAP Kinase substrates.

溶解度

methanol: 0.7 mg/mL;DMSO: 20 mg/mL

其他说明

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.

一般描述

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 p140trk 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.

生化/生理作用

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

重悬

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

警告

Toxicity: Standard Handling (A)