Biological Activity
CRBN-6-5-5-VHL is a cell-permeable and highly potent heterodimerizer comprising E3 ligases recruiting ligands, namely, pomalidomide and VH032-amine th at efficiently knocks down Cereblon (CRBN). CRBN-6-5-5-VHL readily forms heteroternary complex and selectively induces CRBN ubiquitination and proteasomal degradation over VHL in a time- and dose-dependent fashion (0.001 to 1 μM). Higher concentrations (10 μM) causes the degradation of neo-substrates IKZF1 and IKZF3 with no effect on pVHL30 or pVHL19 levels.
