MZ 1, ( )-JQ1 based Degrader (PROTAC) that selectively degrades BRD4, Each

Details:

Cell penetrant Degrader (PROTAC®) compound based on ( )-JQ1 (Cat.No. 4499) conjugated to a von Hippel-Lindau (VHL) ligand. MZ 1 retains high affinity for BRD2, BRD3 and BRD4 bromodomains (Kd = 13-60 nM) but induces preferential degradation of BRD4 over BRD2 and BRD3 (DC50 values for degradation of BRD4 are 8 and 23 nM in H661 and H838 cells, respectively). Exhibits potent cytotoxicity and antiproliferative effects in AML cell lines (pEC50 = 7.6 in Mv4-11 cells). Negative control cis MZ 1 also available. PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.