PD 98059 Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
Beschreibung
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 IC
50 value of 2-7 μM but does not inhibit Raf-activated MAP2K1. It inhibits Raf activation of MAP2K2 with an IC
50 value of 50 μM. PD 98059 also phosphorylates and activates AMP-activated protein kinase (AMPK) in a dose-dependent manner (EC
50 = 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).
Verwenden
PD 98059 is a selective inhibitor of MEK and blocker of MAPK.
Definition
ChEBI: A member of the class of monomethoxyflavones that is 3'-methoxyflavone bearing an additional amino substituent at position 2'
Allgemeine Beschreibung
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; IC
50 = 2 μM); however, it has no effect on NGF-dependent tyrosine phosphorylation of the p140
trk 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.
Biologische Aktivität
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 98059 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
