PD98059

PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM) . PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG) -induced autophagy[1][2][3].

Product Specifications

CAS Number

[167869-21-8]

UNSPSC

12352005

Hazard Statement

H301

Target

Aryl Hydrocarbon Receptor; Autophagy; ERK; MEK

Type

Reference compound

Related Pathways

Autophagy; Immunology/Inflammation; MAPK/ERK Pathway; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PD98059.html

Purity

99.96

Solubility

DMSO : 33.33 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL

Smiles

O=C1C=C(OC2=CC=CC=C21)C3=CC=CC(OC)=C3N

Molecular Formula

C16H13NO3

Molecular Weight

267.28

Precautions

H301

References & Citations

[1]Reiners JJ Jr, et al. PD98059 is an equipotent antagonist of the aryl hydrocarbon receptor and inhibitor of mitogen-activated protein kinase kinase. Mol Pharmacol. 1998 Mar;53 (3) :438-45.|[2]Alessi DR, 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, 1995, 270 (46), 27489-27494.|[3]Di Paola R, et al. PD98059, a specific MAP kinase inhibitor, attenuates multiple organ dysfunction syndrome/failure (MODS) induced by zymosan in mice. Pharmacol Res. 2010 Feb;61 (2) :175-87.|[4]Kojima K, et al. Mitogen-activated protein kinase kinase inhibition enhances nuclear proapoptotic function of p53 in acute myelogenous leukemia cells. Cancer Res. 2007 Apr 1;67 (7) :3210-9.|[5]Kim KY, et al. Inhibition of Autophagy Promotes Salinomycin-Induced Apoptosis via Reactive Oxygen Species-Mediated PI3K/AKT/mTOR and ERK/p38 MAPK-Dependent Signaling in Human Prostate Cancer Cells. Int J Mol Sci. 2017 May 18;18 (5) . pii: E1088.|[6]Jia Luo, et al. DUSP5 (dual-specificity protein phosphatase 5) suppresses BCG-induced autophagy via ERK 1/2 signaling pathway.|[7]Sarah J Parker, et al. Inhibition of TDP-43 accumulation by bis (thiosemicarbazonato) -copper complexes. PLoS One. 2012;7 (8) :e42277.