PROTAC MEK1 Degrader-1, a targeted protein degradation agent, combines a MEK1 inhibitor with a von Hippel-Lindau ligand to effectively inhibit ERK1/2 phosphorylation. With a pIC50 value of 7.0, it exhibits antiproliferative activity against A375 cells [1].

PROTAC MEK1 Degrader-1 (Compound 3) induces MEK1 degradation at concentrations of 1 μM and 10 μM over 12 hours, while lower concentrations increase MEK1 and ERK1/2 expression [1]. At 10 μM, it significantly inhibits IL6 secretion over 12 hours and shows anti-proliferative activity against A375 cells from 0 to 72 hours [1]. Significant MEK and ERK1/2 degradation occurs at 5 hours post-treatment with 10 μM, with complete inhibition at 8 hours [1].