Drug intelligence / Profile preview

PD-98059

Development stage
Preclinical
Modality
Small Molecules
Administration
In Vitro (laboratory Use Only)
01

Overview

PD‑98059 is a synthetic small molecule that acts as a potent and selective inhibitor of mitogen‑activated protein kinase kinases (MAPKK), specifically MEK1 and, to a lesser extent, MEK2. It binds to the inactive form of MEK1/MEK2 and prevents their activation by upstream kinases such as c-Raf. This inhibition blocks the phosphorylation and subsequent activation of MAP kinase (ERK), thereby suppressing downstream signaling in the MAP kinase cascade. PD‑98059 is widely used in research to dissect MAPK pathway functions, including studies on cell proliferation, differentiation, apoptosis, immune responses, and cancer biology. It has demonstrated antiproliferative effects in various cell lines but is not approved for clinical use[1][2][3][4][5].

Other names
2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one2-(2'-amino-3'-methoxyphenyl)oxanaphthalen-4-one4H-1-benzopyran-4-one, 2-(2-amino–3-methoxyphenyl)-2’-Amino–3’-methoxyflavone167869–21–8
02

Targets

MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)AHR (Aryl hydrocarbon receptor)

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