MZ 1
Based on 25 publication(s) in Google Scholar
MZ 1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. Kds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively.
(Pink: BRD4(BD1BD2) ligand (HY-13030); Blue: VHL ligand (HY-125845); Black: linker (HY-140189)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
The MZ 1 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- 純度: 99.86%
- CAS 番号: 1797406-69-9
- 分子式: C49H60ClN9O8S2
- 分子量:1002.64
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保管条件:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 MZ 1
More- Nature. 2023 Jun;618(7963):169-179. [Abstract]
- Mol Cell. 2024 Apr 4;84(7):1304-1320.e16. [Abstract]
- Nat Commun. 2025 May 3;16(1):4133. [Abstract]
- Nat Commun. 2021 Jul 21;12(1):4441. [Abstract]
- Adv Sci (Weinh). 2026 Apr;13(20):e15159. [Abstract]
- Nat Chem Biol. 2024 Dec;20(12):1640-1649. [Abstract]
- Nat Chem Biol. 2023 Dec;19(12):1513-1523. [Abstract]
- J Adv Res. 2025 Jul 4:S2090-1232(25)00504-1. [Abstract]
- J Control Release. 2026 May 10:393:114828. [Abstract]
- Nat Struct Mol Biol. 2024 Feb;31(2):378-389. [Abstract]
- Nat Struct Mol Biol. 2024 Feb;31(2):323-335. [Abstract]
- NPJ Precis Oncol. 2023 Feb 18;7(1):20. [Abstract]
- J Med Chem. 2026 Mar 19. [Abstract]
- J Med Chem. 2024 Apr 25;67(8):6658-6672. [Abstract]
- Biochem Pharmacol. 2025 Jul 12:241:117159. [Abstract]
- Cancer Biol Ther. 2022 Dec 31;23(1):1-15. [Abstract]
- Structure. 2024 Dec 5;32(12):2352-2363.e8. [Abstract]
- ACS Chem Biol. 2019 Oct 18;14(10):2215-2223. [Abstract]
- BMC Cancer. 2024 Feb 16;24(1):220. [Abstract]
- J Immunol. 2021 Jul 15;207(2):493-504. [Abstract]
- Hematology. 2023 Dec;28(1):2247253. [Abstract]
- bioRxiv. 2026 May 5:2026.05.01.722262. [Abstract]
- SSRN. 2025 Jul 8.
- Harvard University. 2023 Mar. 30487357.
- bioRxiv. 2023 Feb 15:2023.02.14.528208. [Abstract]
Customer Validation & Images
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RT-PCR
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WB
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WB
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Flow Cytometry
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Cell Proliferation/Viability Assay
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
Kd: 382/120 nM (BRD4 BD1/2), 119/115 nM (BRD3 BD1/2), 307/228 nM (BRD2 BD1/2)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| EOL1 | IC50 |
1.5 nM
Compound: MZ1; 33
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Antiproliferative activity against human EOL1 cells assessed as inhibition of cell growth
Antiproliferative activity against human EOL1 cells assessed as inhibition of cell growth
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[PMID: 36202064] |
| HeLa | DC50 |
<100 nM
Compound: 7; MZ1
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Protac activity at VHL/BRD4 in human HeLa cells assessed as induction of BRD4 protein degradation incubated for 24 hrs by Western blot analysis
Protac activity at VHL/BRD4 in human HeLa cells assessed as induction of BRD4 protein degradation incubated for 24 hrs by Western blot analysis
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[PMID: 31047748] |
| HL-60 | IC50 |
1.5 nM
Compound: MZ1; 33
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Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth
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[PMID: 36202064] |
| MV4-11 | IC50 |
11.3 nM
Compound: 25; MZ1
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Antiproliferative activity against human MV4-11 cells
Antiproliferative activity against human MV4-11 cells
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[PMID: 35763424] |
MZ 1 conjugates the pan-BET inhibitor JQ1 to VH032, a potent and specific VHL ligand, via a 3-unit PEG linker[2].
MZ 1 (100 and 250 nM; 24 hours) induces BRD4 degradation in LS174t cells 24 h. MZ 1 leads to complete degradation of BRD4 protein, whereas the expression of BRD4 mRNA is not reduced[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LS174t cells
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Concentration:0, 100, and 250 nM
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Incubation Time:24 hours
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Result:Led to complete degradation of BRD4 protein, whereas the expression of BRD4 mRNA was not reduced.
化学情報
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CAS 番号 1797406-69-9
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性状 Solid
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分子量 1002.64
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分子式 C49H60ClN9O8S2
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Color White to light yellow
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SMILES
CC1=C(C)SC2=C1C(C3=CC=C(Cl)C=C3)=N[C@@H](CC(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@@H](O)C4)C(NCC5=CC=C(C6=C(N=CS6)C)C=C5)=O)=O)=O)=O)C7=NN=C(C)N27
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (25)
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Journal Impact Factor
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Most Recent
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Nature
2023 Jun;618(7963):169-179. PMID: 37225982
MZ 1 purchased from MedChemExpress. Usage Cited in: Nature. 2023 Jun;618(7963):169-179. [Abstract]
Effects of c-Myc-RiboTAC and BRD4 degrader MZ1 (0.1 to 10 µM) on the proliferation and apoptosis of HeLa cells upon 48 h treatment (n = 3 biological replicates).
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Mol Cell
Cullin-RING ligases employ geometrically optimized catalytic partners for substrate targeting. [Abstract]2024 Apr 4;84(7):1304-1320.e16. PMID: 38382526 -
Nat Commun
The ESCRT protein CHMP5 promotes T cell leukemia by enabling BRD4-p300-dependent transcription. [Abstract]2025 May 3;16(1):4133. PMID: 40319015
MZ 1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 3;16(1):4133. [Abstract]
qPCR of MYC and EP300 from CT and KD CUTLLl cells treated with 100 nM of the BRD4-PROTAC MZ1 for 4 hours.
MZ 1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 3;16(1):4133. [Abstract]
Western blot of nuclear lysate from CT and KD CUTLL1 cells treated with 100nM of the BRD4-PROTAC MZ1 for 4 hours, with quantification of p300 protein levels relative to CT-MZ1.
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Nat Commun
Stromal induction of BRD4 phosphorylation Results in Chromatin Remodeling and BET inhibitor Resistance in Colorectal Cancer. [Abstract]2021 Jul 21;12(1):4441. PMID: 34290255 -
Adv Sci (Weinh)
2026 Apr;13(20):e15159. PMID: 41637562 -
Nat Chem Biol
2024 Dec;20(12):1640-1649. PMID: 39075252
MZ 1 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2024 Dec;20(12):1640-1649. [Abstract]
Western blot of BRD4 degradation in K562 cells that were treated with DMSO or different concentrations (1, 10, 100 nM) of MMH1, MMH2, dBET6 or MZ1 for 6 h.
MZ 1 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2024 Dec;20(12):1640-1649. [Abstract]
Flow cytometry analysis of BRD4BD2-eGFP degradation in K562 cells that were treated with increasing concentrations of MMH1, MMH2, dBET6 or MZ1 for 2 h, 6 h, or 16 h (n = 3).
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Nat Chem Biol
2023 Dec;19(12):1513-1523. PMID: 37653169 -
J Adv Res
2025 Jul 4:S2090-1232(25)00504-1. PMID: 40617410 -
J Control Release
The HSP90-dependent bioorthogonal PROTAC prodrug system enables tumor-selective and enhanced protein degradation. [Abstract]2026 May 10:393:114828. PMID: 41839264 -
Nat Struct Mol Biol
Mechanism of millisecond Lys48-linked poly-ubiquitin chain formation by cullin-RING ligases. [Abstract]2024 Feb;31(2):378-389. PMID: 38326650 -
Nat Struct Mol Biol
2024 Feb;31(2):323-335. PMID: 38177676 -
NPJ Precis Oncol
Targeting ACE2-BRD4 crosstalk in colorectal cancer and the deregulation of DNA repair and apoptosis. [Abstract]2023 Feb 18;7(1):20. PMID: 36801948 -
J Med Chem
2026 Mar 19. PMID: 41852276 -
J Med Chem
Peptide Inhibitor Targeting the Extraterminal Domain in BRD4 Potently Suppresses Breast Cancer Both In Vitro and In Vivo. [Abstract]2024 Apr 25;67(8):6658-6672. PMID: 38569135 -
Biochem Pharmacol
Discovery of a potent BRD4 PROTAC and evaluation of its bioactivity in breast cancer cell lines. [Abstract]2025 Jul 12:241:117159. PMID: 40659131 -
Cancer Biol Ther
BRD4 PROTAC degrader MZ1 exerts anticancer effects in acute myeloid leukemia by targeting c-Myc and ANP32B genes. [Abstract]2022 Dec 31;23(1):1-15. PMID: 36170346 -
Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062 -
ACS Chem Biol
Cellular Resistance Mechanisms to Targeted Protein Degradation Converge Toward Impairment of the Engaged Ubiquitin Transfer Pathway. [Abstract]2019 Oct 18;14(10):2215-2223. PMID: 31553577
MZ 1 purchased from MedChemExpress. Usage Cited in: ACS Chem Biol. 2019 Oct 18;14(10):2215-2223. [Abstract]
Immuno-blots of six cell lines, treated for 5 h with either DMSO or different concentrations of the degraders MZ1 and dBet6.
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BMC Cancer
MZ1, a BRD4 inhibitor, exerted its anti-cancer effects by suppressing SDC1 in glioblastoma. [Abstract]2024 Feb 16;24(1):220. PMID: 38365636 -
J Immunol
Proteolysis-Targeting Chimeras Enhance T Cell Bispecific Antibody-Driven T Cell Activation and Effector Function through Increased MHC Class I Antigen Presentation in Cancer Cells. [Abstract]2021 Jul 15;207(2):493-504. PMID: 34215653 -
Hematology
BRD4 PROTAC degrader MZ1 exhibits anti-B-cell acute lymphoblastic leukemia effects via targeting CCND3. [Abstract]2023 Dec;28(1):2247253. PMID: 37594294 -
bioRxiv
2026 May 5:2026.05.01.722262. PMID: 42146509 -
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bioRxiv
Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders. [Abstract]2023 Feb 15:2023.02.14.528208. PMID: 36824856
溶剤 & 溶解度
DMSO : 100 mg/mL (99.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (272 KB)
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SDS (643 KB)
- English - EN (643 KB)
- Français - FR (643 KB)
- Deutsch - DE (643 KB)
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- Español - ES (643 KB)
- Swedish - SV (643 KB)
- Italian - IT (643 KB)
- Korean - KR (643 KB)
- Portuguese - PT (643 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Zengerle M, et al. Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4. ACS Chem Biol. 2015 Aug 21;10(8):1770-7. [Content Brief]
[2]. Gadd MS, et al. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 May;13(5):514-521. [Content Brief]
[3]. Otto C, et al. Targeting bromodomain-containing protein 4 (BRD4) inhibits MYC expression in colorectal cancer cells. Neoplasia. 2019 Nov;21(11):1110-1120. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9974 mL | 4.9868 mL | 9.9737 mL | 24.9342 mL |
| 5 mM | 0.1995 mL | 0.9974 mL | 1.9947 mL | 4.9868 mL | |
| 10 mM | 0.0997 mL | 0.4987 mL | 0.9974 mL | 2.4934 mL | |
| 15 mM | 0.0665 mL | 0.3325 mL | 0.6649 mL | 1.6623 mL | |
| 20 mM | 0.0499 mL | 0.2493 mL | 0.4987 mL | 1.2467 mL | |
| 25 mM | 0.0399 mL | 0.1995 mL | 0.3989 mL | 0.9974 mL | |
| 30 mM | 0.0332 mL | 0.1662 mL | 0.3325 mL | 0.8311 mL | |
| 40 mM | 0.0249 mL | 0.1247 mL | 0.2493 mL | 0.6234 mL | |
| 50 mM | 0.0199 mL | 0.0997 mL | 0.1995 mL | 0.4987 mL | |
| 60 mM | 0.0166 mL | 0.0831 mL | 0.1662 mL | 0.4156 mL | |
| 80 mM | 0.0125 mL | 0.0623 mL | 0.1247 mL | 0.3117 mL |
MZ 1 関連分類
HY-107425 関連分類
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