MZ1 | BRD4 degrader

MZ1 Chemical structure

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MZ1 (1797406-69-9) consists of JQ1 tethered to a ligand for the E3 ubiquitin ligase VHL and is a selective degrader of the BET bromodomain protein BRD4. It rapidly and potently induces reversible, long-lasting and unexpectedly selective degradation of BRD4 over BRD2 and BRD3.1 It exerts anticancer effects in acute myeloid leukemia by targeting c-Myc and ANP32B.2 An important tool for studying the effects of BRD4 degradation in cancer therapy.3

References/Citations:

  1. Zengerle et al. (2015), Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4; ACS Chem. Biol. 10 1770
  2. Ma et al. (2022), BRD4 PROTAC degrader MZ1 exerts anticancer effects in acute myeloid leukemia by targeting c-Myc and ANP32B genes; Cancer Biol. Ther. 23 1
  3. Zhou et al. (2022), A comprehensive review of BET-targeting PROTACs for cancer therapy; Bioorg. Med. Chem. 73 117033
1797406-69-9, BRD4 degrader, BRD4 protac, MZ1, MZ1 supplier

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Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

MZ1 (1797406-69-9) consists of JQ1 tethered to a ligand for the E3 ubiquitin ligase VHL and is a selective degrader of the BET bromodomain protein BRD4. It rapidly and potently induces reversible, long-lasting and unexpectedly selective degradation of BRD4 over BRD2 and BRD3.1 It exerts anticancer effects in acute myeloid leukemia by targeting c-Myc and ANP32B.2 An important tool for studying the effects of BRD4 degradation in cancer therapy.3

References/Citations:

  1. Zengerle et al. (2015), Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4; ACS Chem. Biol. 10 1770
  2. Ma et al. (2022), BRD4 PROTAC degrader MZ1 exerts anticancer effects in acute myeloid leukemia by targeting c-Myc and ANP32B genes; Cancer Biol. Ther. 23 1
  3. Zhou et al. (2022), A comprehensive review of BET-targeting PROTACs for cancer therapy; Bioorg. Med. Chem. 73 117033