ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC 50 s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D , respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis.
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