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

MZ 1 

Cat. No.: HY-107425 Purity: 98.51%
Handling Instructions

MZ 1 is a PROTAC BRD4 degrader. 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.

For research use only. We do not sell to patients.

MZ 1 Chemical Structure

MZ 1 Chemical Structure

CAS No. : 1797406-69-9

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1 mg USD 60 In-stock
Estimated Time of Arrival: December 31
5 mg USD 200 In-stock
Estimated Time of Arrival: December 31
10 mg USD 380 In-stock
Estimated Time of Arrival: December 31
50 mg USD 715 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE MZ 1

    MZ 1 purchased from MCE. Usage Cited in: ACS Chem Biol. 2019 Oct 18;14(10):2215-2223.

    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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    Description

    MZ 1 is a PROTAC BRD4 degrader. 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].

    IC50 & Target

    Kd: 382/120 nM (BRD4 BD1/2), 119/115 nM (BRD3 BD1/2), 307/228 nM (BRD2 BD1/2)[1].

    In Vitro

    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].

    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.
    Molecular Weight

    1002.64

    Formula

    C₄₉H₆₀ClN₉O₈S₂

    CAS No.

    1797406-69-9

    SMILES

    CC1=C(C)SC2=C1C(C3=CC=C(Cl)C=C3)=N[[email protected]@H](CC(NCCOCCOCCOCC(N[[email protected]@H](C(C)(C)C)C(N4[[email protected]@H](C[[email protected]@H](O)C4)C(NCC5=CC=C(C6=C(N=CS6)C)C=C5)=O)=O)=O)=O)C7=NN=C(C)N27

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (24.93 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (2.49 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (2.49 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 98.51%

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    Keywords:

    MZ 1MZ1MZ-1PROTACEpigenetic Reader DomainProteolysis-targeting chimeraselectiveproteindegradationBRD4DegraderLS174tcellsInhibitorinhibitorinhibit

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