MZ-1

MZ-1 (CAS No.: 1797406-69-9) is a heterobifunctional small-molecule probe for targeted protein degradation research, classified as a BET family-targeting degrader. Based on the PROTAC strategy, it is composed of a JQ1-derived BET bromodomain ligand conjugated via a linker to a VHL E3 ubiquitin ligase-recruiting ligand, enabling formation of the VHL–MZ?1–BRD4 ternary complex, thereby inducing substrate ubiquitination and selective clearance of BRD4 through the proteasomal pathway; under higher exposure conditions, it may also affect BRD2 and BRD3. As a chemical biology tool, it is suitable for elucidating dependencies in epigenetic and transcriptional regulation and their network hierarchy. In vitro studies have shown that MZ?1 has nanomolar-level binding ability to BET bromodomains and can induce rapid and selective BRD4 degradation in cellular systems at submicromolar to low micromolar concentrations; this effect can typically be observed within several hours and maintained in the presence of continued compound exposure. Typical applications include target validation in cell models, pathway mapping, genetic or pharmacological synergy studies, as well as phenotypic and high-content screening across multiple cell lines; in exploratory studies in animal models, it may also be used to evaluate the impact of BRD4 removal on molecular phenotypes and functional readouts. Specific experimental concentrations and exposure regimens should be optimized according to research objectives and experimental design. This product is for laboratory research use only and must not be used for human or animal ingestion, or for medical, clinical, or diagnostic-related purposes.