TD-165 is a PROTAC-based cereblon (CRBN) degrader. TD-165 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group[1].
TD-165 (0-100 nM; 24 hours) shows 50% degradation concentration (DC50) and maximum degradation (Dmax) value of 20.4 nM and 99.6%, respectively[1].TD-165 (0.1-10 μM; 24 hours) leads to a concentration-dependent decrease in the level of CRBN proteins in HEK293T cells[1].
[1]. Kim K, et al. Disordered region of cereblon is required for efficient degradation by proteolysis-targeting chimera.Sci Rep. 2019 Dec 23;9(1):19654.