MZ1 is a cell penetrant Proteolysis Targeting Chimera (PROTAC) compound based on (+)-JQ1 conjugated to a von Hippel-Lindau (VHL) ligand. It 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). MZ1 exhibits potent cytotoxicity and anti-proliferative effects in AML cell lines (pEC50 = 7.6 in Mv4-11 cells).
|Quantity||1 mg, 5 mg|
|Molecular Weight||1002.64 g/mol|
|Physical State||Lyophilized white to off-white solid|
|Solubility||100 mg/mL in DMSO; 100 mg/ml in ethanol|
|Storage||solutions at -80°C; desiccated at -20°C, avoid freeze/thaw cycles|