Figure 5.
Evaluation of the mechanism of action of BET degradation induced by 35 (QCA570). RS4;11 cells were pre-treated for 2 h with DMSO, BET inhibitor 22 (10 μM), cereblon ligand Lenalidomide (10 μM), E1 neddylation inhibitor MLN4924 (1 μM), or proteasome inhibitors MG-132 (20 μM) and Carfilzomib (0.1 μM). Cells were then treated for 3 h with BET degrader 35 (QCA570) at 0.5 nM, a concentration that induces complete degradation of all BET-BRD proteins and downregulation of c-Myc.