MZP-54 is a PROTAC targeting on BET, consist of a warhead I-BET726 (BET bromodomain inhibitor) linked to a VHL ligand VH032. It exhibited affinity to the Brd4BD2 and VHL-EloC-EloB protein with Kd values of 4nM and 105nM, respectively. Treatment with 50nM MZP-54 for 4h led to degradation of Brd4 by 87%, accompanied with the downregulation of c-MYC by 73% in MV4;11 cells.
Structure of 2010159-47-2
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