INY-06-061 is a potent and selective heterobifunctional degrader of ERK5 with binding Kd of 12 nM and DC50 of 21 nM in MOLT4 cells (5h treatment).
INY-06-061 displays a similar selectivity profile to both the parental inhibitor INY-06-086 and the original ERK5 inhibitor BAY-885.
INY-06-061-induced ERK5 degradation is dependent on the ubiquitin-proteasome system.
INY-06-061 treatment does not compromise viability in multiple cancer cell lines, does not affect pro-inflammatory cytokine secretion in endothelial cells.
