2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. MZ 1

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.

CAS 番号 : 1797406-69-9

容量 価格（税別） 在庫状況 数量
1 mg $60 在庫あり
5 mg $200 在庫あり
10 mg $260 在庫あり
25 mg $400 在庫あり
50 mg $520 在庫あり
100 mg $740 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 24 publication(s) in Google Scholar

Other Forms of MZ 1:

MZ 1 関連抗体

Top Publications Citing Use of Products

    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.

    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).

    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).

    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.

    PROTACs アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

    Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Brd BRPF1 BRPF2 BRPF3 BRD2 BRD3 BRD4 BRDT CECR2 BD1 BD2 BRD7 BRD9 BET BAZ

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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[1]. (Pink: BRD4(BD1BD2) ligand (HY-13030); Blue: VHL ligand (HY-125845); Black: linker (HY-140189)).

    IC50 & Target

    Kd: 382/120 nM (BRD4 BD1/2), 119/115 nM (BRD3 BD1/2), 307/228 nM (BRD2 BD1/2)[1].
    Cellular Effect
    Cell Line Type Value Description References
    EOL1 IC50
    1.5 nM
    Compound: MZ1; 33
    Antiproliferative activity against human EOL1 cells assessed as inhibition of cell growth
    Antiproliferative activity against human EOL1 cells assessed as inhibition of cell growth
    		[PMID: 36202064]
    HeLa DC50
    <100 nM
    Compound: 7; MZ1
    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
    		[PMID: 31047748]
    HL-60 IC50
    1.5 nM
    Compound: MZ1; 33
    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
    		[PMID: 36202064]
    MV4-11 IC50
    11.3 nM
    Compound: 25; MZ1
    Antiproliferative activity against human MV4-11 cells
    Antiproliferative activity against human MV4-11 cells
    		[PMID: 35763424]
    体外実験

    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.

    MZ 1 関連抗体

    Western Blot Analysis[3]

    Cell Line: LS174t cells
    Concentration: 0, 100, and 250 nM
    Incubation Time: 24 hours
    Result: Led to complete degradation of BRD4 protein, whereas the expression of BRD4 mRNA was not reduced.
    分子量

    1002.64

    分子式

    C49H60ClN9O8S2
    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    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
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    -20°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
    溶剤 & 溶解度
    体外: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.9974 mL 4.9868 mL 9.9737 mL
    5 mM 0.1995 mL 0.9974 mL 1.9947 mL
    10 mM 0.0997 mL 0.4987 mL 0.9974 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    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.

    • Protocol 1

      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.
    • Protocol 2

      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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: 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)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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

    純度: 99.86%

    COA (244 KB) HNMR (157 KB) RP-HPLC (162 KB) LCMS (234 KB)

    取扱説明書 (2659 KB)
    参考文献

    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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    MZ 1 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    MZ 11797406-69-9MZ1MZ-1PROTACsEpigenetic Reader DomainselectiveproteindegradationBRD4DegraderLS174tcellsInhibitorinhibitorinhibit

    最近チェックした製品:

    オンラインお問い合わせ

    Your information is safe with us. * Required Fields.

    製品名

    		  

    カスタマ需要量 *

    お名前 *

    		 

    タイトル

    メールアドレス *

    		 

    電話番号 *

    デパートメント

    		 

    組纖名 *

    市区町村

    都道府県

    国或いは地域 *

    		      

    必ず会社名を記載ください。個人への返信は行いません。

    備考

    バルクお問い合わせ

    Inquiry Information

    製品名:
    MZ 1
    製品番号:
    HY-107425
    数量:
    MCE 日本正規代理店:

    カスタマーレビュー

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    製品名

    		  

    Lot #

    お名前 *

    		 

    メールアドレス *

    電話番号 *

    		 

    部門 *

    組纖名 *

    		 

    国或いは地域 *

    備考

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.