2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one

개요PD 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).

용도PD 98059 is a selective inhibitor of MEK and blocker of MAPK.

일반 설명Selective, 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.