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MEK

MEK inhibitors act on mitogen-activated protein kinase kinases 1 and 2 (MEK1, MEK2) in growth factor signaling. MEK was cloned in 1992 as a protein kinase that phosphorylates the product of the extracellular signal-regulated kinase (ERK) gene. It is a dual-specificity enzyme that activates ERK1 and ERK2 by phosphorylating a threonine and a tyrosine residue. PD98059, reported in 1995, and U0126, reported in 1998 and listed as U0126-EtOH, were early synthetic MEK inhibitors. Trametinib, cobimetinib and binimetinib are allosteric MEK1/2 inhibitors used in studies of Ras- and Raf-driven signaling. (E/Z)-BIX 02189 instead targets MEK5, the kinase that activates ERK5. Inhibitors of the downstream kinases are listed in the sibling category ERK.

Cat. No.

A10705

CAS No.

167869-21-8

PD98059

PD98059 is an equipotent antagonist of the aryl hydrocarbon receptor and inhibitor of mitogen-activated protein kinase kinase.

In stock View Details

5 mg

$25.00

10 mg

$40.00

All 8 sizes