Potent and selective ERK5 inhibitor (IC50
= 8 nM). Exhibits >1,000-fold selectivity for ERK5 over a panel of over 200 kinases. Also exhibits selectivity over bromodomain BRD4 (Kd
= 3,600 nM). Increases vomocytosis in human macrophages in vitro
, as well as in an in vivo
zebrafish model of cryptococcal disease, reducing spread of infection.
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All Tocris products are intended for laboratory research use only.
ERK5 kinase activity is dispensable for cellular immune response and proliferation.
Lin et al.
Vomocytosis of live pathogens from macrophages is regulated by the atypcial MAP kinase ERK5.
Gilbert et al.
Science Advances, 2017;3:e1700898