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  • PD 98059
  • 產品型號:101-167869-21-8

    商品規格:

    商品售價

Cell-permeable, selective & reversible inhibitor of MAP Kinase Kinase (MEK). Inhibits MAP Kinase activation and subsequent phosphorylation of MAP Kinase substrates.

Synonym: 2'-Amino-3'-methoxyflavone, MEK Inhibitor V

>99%
C16H13NO3
M.W. 267.28

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 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.

Solubility: Soluble in DMSO at 25 mg/mL; soluble in ethanol at 1 mg/mL with warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 50-100 µM

Potent, selective and cell-permeable inhibitor of MAP kinase kinase (also known as MAPK/ERK kinase or MEK kinase). Inhibits phosphorylation of MAP kinase by MAP kinase kinase. PD 98059 does not inhibit MAP kinase itself. IC50 values for PD 98059-induced effects are in the 1-20 µM range for many assays; it is somewhat weaker in inhibiting cell growth in monolayers or agar for some cell lines. Dudley, D.T., et al. "A synthetic inhibitor of the mitogen-activated protein kinase cascade." "Proc. Natl. Acad. Sci. USA 92: 7686-7689 (1995). Pang, L., et al. "Inhibition of MAP kinase kinase blocks the differentiation of PC-12 cells induced by nerve growth factor." J. Biol. Chem. 270: 13585-13588 (1995). Waters, S.B., et al. "Desensitization of Ras activation by a feedback disassociation of the SOS-Grb2 complex." J. Biol. Chem. 270: 20883-20886 (1995). Langlois, W.J., et al. "Negative feedback regulation and desensitization of insulin- and epidermal growth factor-stimulated p21ras activation." J. Biol. Chem. 270: 25320-25323 (1995). Alessi, D.R., et al. "PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo." J. Biol. Chem. 270: 27489-27494 (1995).

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