PD98059 Inhibitor CAS No. 167869-21-8

Cat. No.	Name	Size	Price
KI1362	PD98059	10 mg	$234
	PD98059	50 mg	$752
	PD98059	200 mg	$1072

Chemical Characteristic

Product Name	PD98059
CAS No.	167869-21-8
Molecular Weight	267.28
Formula	C₁₆H₁₃NO₃
Chemical Name	2-(2-amino-3-methoxyphenyl)-4H-chromen-4-one
Smiles	c1(cc(=O)c2c(o1)cccc2)c1c(c(ccc1)OC)N
Chemical Structure

Biological activities

PD98059 is a specific inhibitor of mitogen-activated protein kinase kinase (MEK). The IC50 of PD98059 is 1 µM against aryl hydrocarbon receptor (AHR) transformation. PD98059 results in a rapid loss (>95%) of the dually phosphorylated forms of extracellular signal-regulated kinase with an IC50 of 1 µM. ^[1] PD98059 completely blocks the TPA (12-O-tetradecanoylphorbol-13-acetate)-induced differentiation of ML-1 cells.^[2] PD98059 at the doses of 10 and 40 µM significantly inhibits (15% and 64%) myogenic tone. PD98059 also significantly reduces the vasopressin (0.1 µM)- and KCl (60 mM)-induced tone.^[3] Microinfusion of 50 µM PD98059 also significantly decreases the phosphorylation of Elk-1 (to 59.2% of control conditions).^[4] PD98059 prevents not only basal and Aβ-induced MAPK activation but also neurite degeneration induced by fibrillar Aβ in mature hippocampal neurons.^[5]

Protocols

In vitro: PD98059 is dissolved in dimethyl sulfoxide to a concentration of 100 mM and stored at -80 °C.^[5]

References

[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, 53(3): 438-445. [2] He H, et al. Phorbol ester-induced mononuclear cell differentiation is blocked by the mitogen-activated protein kinase kinase (MEK) inhibitor PD98059. Cell Growth Differ. 1999, 10(5): 307-315. [3] Lagaud GJ, et al. Nonspecific inhibition of myogenic tone by PD98059, a MEK1 inhibitor, in rat middle cerebral arteries. Biochem Biophys Res Commun. 1999, 257(2): 523-527. [4] Strohm C, et al. Inhibition of the ER-kinase cascade by PD98059 and UO126 counteracts ischemic preconditioning in pig myocardium. J Cardiovasc Pharmacol. 2000, 36(2): 218-229. [5] Rapoport M, et al. PD98059 prevents neurite degeneration induced by fibrillar beta-amyloid in mature hippocampal neurons. J Neurochem. 2000, 74(1): 125-133.

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