PD-98059 is an oxanaphthalenone-based inhibitor of MAPK-activating enzyme, MAPK/ERK kinase (MEK), without significant inhibitory activity of MAPK itself. [1] PD-98059 does not inhibit Raf-activated MAPKK1, but rather prevents activation of MAPKK1 by Raf or MEK kinase in vitro at IC50 values of 2-7 uM. [2]
Exposure of MCF10A human breast epithelial cells resulted in a rapid loss of dually phosphorylated forms of extracellular signal-regulated kinase at an IC50 of 1 uM. PD-98059 is believed to be a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist at concentrations commonly used to inhibit MEK at the signalling processes that entail MEK activation. [3]
PD-98059 has also been shown to dramatically reduce hypoxia-induced transcription of HRE-driven reporter gene more so than that of endogenous VEGF and EPO. [4]
Technical information:
| Chemical Formula: | C16H13NO3 | |
| CAS #: | 167869-21-8 | |
| Molecular Weight: | 267.28 | |
| Purity: | >98% | |
| Appearance: | Yellow | |
| Chemical Name: | 2-(2-amino-3-methoxyphenyl)-4H-chromen-4-one | |
| Solubility: | Up to 75 mM in DMSO | |
| Synonyms: | PD-98059, PD 98059, PD98059 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Dudley et al., A synthetic inhibitor of the mitogen-activated protein kinase cascade. Proc. Natl. Acad. Sci. 1995, 92(17), 7686-7689. Pubmed ID: 7644477 |
| 2. | Alessi 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. Pubmed ID: 7499206 |
| 3. | Reiners et al., PD98059 is an equipotent antagonist of the aryl hydrocarbon receptor and inhibitor of mitogen-activated protein kinase kinase. Mol. Pharmacol. 1998, 53(3), 438-445. Pubmed ID: 9495809 |
| 4. | Hur et al., Mitogen-activated protein kinase kinase inhibitor PD98059 blocks the trans-activation but not the stabilization or DNA binding ability of hypoxia-inducible factor-1alpha. Mol. Pharmacol. 2001, 59(5), 1216-1224. Pubmed ID: 7499206 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
