Selective MEK5 and ERK5 inhibitor (IC50
values are 1.5 and 59 nM respectively). Inhibits sorbitol-induced ERK5 phosphorylation in HeLa cells. Selective for MEK5 and ERK5 over MEK1/2, ERK1/2 and a panel of 87 kinases. Induces apoptosis in acute myeloid leukemia tumor cells.
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Identification of pharmacological inhibitors of the MEK5/ERK5 pathway.
Tatake et al.
Extracellular-signal-regulated kinase 5 modulates the antioxidant response by transcriptionally controlling Sirtuin 1 expression in leukemic cells.
Lopez-Royuela et al.
Int.J.Biochem.Cell Biol., 2014;53:253
Targeted deletion of the extracellular signal-regulated protein kinase 5 attenuates hypertrophic response and promotes pressure overload-induced apoptosis in the heart.
Kimura et al.