PD98059 is a non-ATP competitive MEK inhibitor with an IC50 of 2 μM in a cell-free assay and specifically inhibits MEK-1 mediated MAPK activation. It did not directly inhibit ERK1 or ERK2. PD98059 is a ligand and antagonist of aryl hydrocarbon receptor (AHR).

 

Brand: BCM

 

Target: ERK; Aryl Hydrocarbon Receptor; MEK; Autophagy

 

Signaling Pathways: Autophagy; Immunology/Inflammation; MAPK

 

In Vitro: PD 098059 does not inhibit Raf-activated MAPKK1 but that it prevents the activation of MAPKK1 by Raf or MEK kinase in vitro at concentrations (IC50: 2-7 μM). PD 098059 also acts as a specific inhibitor of the activation of MAPKK in Swiss 3T3 cells, suppressing by 80-90% its activation by a variety of agonists. Concentrations of PD98059 of </=20 μM were not cytotoxic to cultures of the immortalized human breast epithelial cell line MCF10A. The agent was weakly cytostatic at concentrations of >/=10 μM. In vivo exposure of cultures to </=20 microM PD98059 for 2-22 hr did not affect overall extracellular signal-regulated kinase contents; however, exposure to PD98059 resulted in a rapid loss (>95%) of the dually phosphorylated forms of the extracellular signal-regulated kinase (IC50: 1 μM) .

 

Melting Point: 164～165℃

 

Boiling Point: 453.1±45.0 °C(Predicted)

 

pKa: 1.21±0.10(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; Insoluble in Ethanol.

 

GHS: GHS07

 

Isomeric SMILES: COC1=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2  

 

InChIKey: QFWCYNPOPKQOKV-UHFFFAOYSA-N  

 

InChI: InChI=1S/C16H13NO3/c1-19-14-8-4-6-11(16(14)17)15-9-12(18)10-5-2-3-7-13(10)20-15/h2-9H,17H2,1H3

 

Attribute
[Chem Name]	2-(2-amino-3-methoxyphenyl)chromen-4-one
[Synonym]	PD98059
[CAS No.]	167869-21-8
[MDL No.]	MFCD00671789
[Formula]	C16H13NO3
[Molecular]	267.28
[Form]	Yellow solid
[Storage]	Sealed in dry. Store in freezer, under -20°C

Goods Tag