Extracellular signal-regulated kinase 5 (ERK5), a member of the mitogen-activated protein kinase (MAPK) family, is ubiquitously expressed in mammalian tissues and cell types, where it is activated by extracellular stimuli, including several growth factors and cellular stresses[1]. ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively[2]. An anti-angiogenic effect was apparent with Matrigel plugs from mice treated with ERK5-IN-2 (100 mg/kg, p.o.) twice daily for 7 days[2]. In a human tumour xenograft model (A2780 cells), ERK5-IN-2 (100 mg/kg, p.o.) treatment twice-daily for 10 days led to significant tumour volume reduction by 57% when compared to the control group[2].
搜索
