PD98059PD98059
MedChemExpress (MCE)
HY-12028
167869-21-8
99.96%
4°C, protect from light *In solvent : -80°C, 1 year
-20°C, 6 months (protect from light)
Room temperature in continental US
may vary elsewhere.
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.
PD98059 (20 μM
24 hours) causes G1-phase cell cycle arrest in OCI-AML-3 cells[4]. PD98059 (10 μM
22 hours) results in concentration-dependent reductions in the dually phosphorylated forms of ERK1 and ERK2[1]. PD98059 both prevents ERK activation and blocks formation of TDP-43 and HuR-positive SGs[7].
PD98059 (10 mg/kg
i.p.
1 and 6 hours after Zymosan) significantly reduces the level of p-ERK1/2 in zymosan-injected mice[3].
MEK1 2-7 μM (IC50) MEK2 50 μM (IC50) ERK1 ERK2 Autophagy
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[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. [Content Brief]
[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. [Content Brief]
[3]. Jia Luo, et al. DUSP5 (dual-specificity protein phosphatase 5) suppresses BCG-induced autophagy via ERK 1/2 signaling pathway.
[4]. 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. [Content Brief]
[5]. 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. [Content Brief]
[6]. 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. [Content Brief]
[7]. Sarah J Parker, et al. Inhibition of TDP-43 accumulation by bis(thiosemicarbazonato)-copper complexes. PLoS One. 2012
7(8):e42277. [Content Brief]