MZ1 | BRD4 degrader

CAS:
 1797406-69-9
Catalog Number:
 10-5090
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
CAS:
1797406-69-9
Catalog Number:
10-5090
Activity:
BRD4 degrader
Chemical Names:
(2S,4R)-1-((S)-2-(tert-Butyl)-17-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,16-dioxo-6,9,12-trioxa-3,15-diazaheptadecan-1-oyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Molecular Weight:
1002.64
Molecular Formula:

C49H60ClN9O8S2

Solubility:
Soluble in DMSO (100 mg/ml with warming)
Physical Properties:
Pale yellow solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

Safety Data Sheet:

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Product Data Sheet:

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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

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