PPM-3, a selective PROTAC ERK5 degrader, exhibits a potent inhibitory concentration (IC 50) of 62.4 nM. While not directly inhibiting tumor cell growth, PPM-3 affects tumor progression through influencing macrophage differentiation [1].

ERK5:62.4 nM

PPM-3, applied at a concentration of 200 nM for 0-72 hours to A375 cells, initiates ERK5 degradation within 2-4 hours, with peak degradation observed at 12 hours and sustained for at least 72 hours [1]. Additionally, PPM-3, ranging from 0-1 μM for 12 hours, exhibits ERK5 degradation activity in various cancer cell lines—H1975, HepG2, MDA-MB-231, PC-3, HCT116, and A375—with respective DC50 values of 11.5±2.5, 13.7±8.2, 22.7±13.3, 23.5±10.3, 5.6±1.9, and 41.4±22.3 nM [1].