Skip to main content
. Author manuscript; available in PMC: 2019 Aug 9.
Published in final edited form as: J Med Chem. 2018 Jul 18;61(15):6685–6704. doi: 10.1021/acs.jmedchem.8b00506

Figure 5.

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.