Specifications
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).
Info
| Purity | >98.0% |
| 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 |
| CAS No. | 1797406-69-9 |
| Storage | solutions at -80°C; desiccated at -20°C, avoid freeze/thaw cycles |
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