MZ1

**MZ1** is a proteolysis-targeting chimera (PROTAC) designed as a selective degrader of bromodomain-containing protein 4 (BRD4), composed of a JQ1-derived bromodomain inhibitor linked via a PEG linker to a von Hippel-Lindau (VHL) E3 ubiquitin ligase ligand. It recruits the VHL ligase to ubiquitinate and proteasomally degrade BRD4 (and to a lesser extent BRD2/BRD3), disrupting BET protein-mediated transcriptional regulation of oncogenes. Developed as a research tool by academic groups, MZ1 has demonstrated potent anti-proliferative, pro-apoptotic, and anti-invasive effects in preclinical cancer models including glioblastoma (GBM), acute myeloid leukemia (AML), B-cell acute lymphoblastic leukemia (B-ALL), neuroblastoma (NB), breast cancer (notably HER2+ where it synergizes with trastuzumab), and ovarian cancer, with in vivo efficacy in xenograft models via cell cycle arrest (G2/M), DNA damage induction, and suppression of pathways like EMT, E2F targets, and KRAS signaling.

Other names

BET PROTACBET PROTAC MZ-1