167869-21-8

PD 98059 is a noncompetitive inhibitor of the MAPK pathway. It prevents the activation of MEK by Raf or MEK kinase (a MAP3K) with an IC₅₀ value of 2-7 μM but does not inhibit Raf-activated MAP2K1. It inhibits Raf activation of MAP2K2 with an IC₅₀ value of 50 μM. PD 98059 also phosphorylates and activates AMP-activated protein kinase (AMPK) in a dose-dependent manner (EC₅₀ = 35 μM in HEK293 cells). It increases the ratios of ADP to ATP and AMP to ATP and increases phosphorylation of the AMPK target acetyl-CoA carboxylase (ACC).

A selective inhibitor of MEK and blocker of MAP

ChEBI: A member of the class of monomethoxyflavones that is 3'-methoxyflavone bearing an additional amino substituent at position 2'

Specific inhibitor of mitogen-activated protein kinase kinase (MAPKK / MEK). Acts by binding to the inactivated form of MEK, thereby preventing its phosphorylation by cRAF or MEK kinase (IC 50 = 2-7 μ M). Inhibits cell growth and proliferation in acute myelogenous leukemia (AML) cell lines; causes G 1 arrest by blocking p53-dependent p21 induction. Also available as part of the MAPK Cascade Inhibitor Tocriset™ and MAPK Inhibitor Tocriset™ .

PD 98,059 is a flavonoid and specific inhibitor of mitogen-activated protein kinase kinase (MAPKK). In mice, PD 98,059 helps to block zymosan stimulated organ dysfunction syndrome and non-septic shock. It is known to inhibit in vitro hypertrophy. PD 98,059 also induces cartilage formation in mesenchymal stromal cells.

4°C, protect from light

1) Alessi et al. (1995), 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 2) Dudley et al. (1995), A synthetic inhibitor of the mitogen-activated protein kinase cascade; Proc. Natl. Acad. Sci., 92 7686 3) Hotokezaka et al. (2002) U0126 and PD98059, specific inhibitors of MEK, accelerate differentiation of RAW264.7 cells into osteoclast-like cells; J. Biol. Chem., 277 47366 4) Xiaoxia et al. (2004) BMP4 supports self-renewal of embryonic stem cells by inhibiting mitogen-activated protein kinase pathways; Proc. Natl. Acad. Sci. USA 101 6027