1. PROTAC
    Epigenetics
  2. PROTAC
    Epigenetic Reader Domain
  3. MZP-54

MZP-54 

Cat. No.: HY-112376 Purity: 98.05%
Handling Instructions

MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2.

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

MZP-54 Chemical Structure

MZP-54 Chemical Structure

CAS No. : 2010159-47-2

Size Price Stock Quantity
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1600 In-stock
Estimated Time of Arrival: December 31
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100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2.

IC50 & Target[1]

VHL

 

BRD4 BD2

4 nM (Kd)

In Vitro

MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2. MZP-54 binds to VHL-EloC-EloB protein (VCB) with a Kd of 105 ± 24 nM. MZP-54 shows an inhibitory activity against MV4;11 and HL60 cells, with pEC50s of 7.08 ± 0.05 and 6.37 ± 0.03, respectively. MZP-54 also exhibits high depletion of cMyc levels[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

1036.67

Formula

C₅₅H₆₆ClN₇O₉S

CAS No.

2010159-47-2

SMILES

O=C(NCCOCCOCCOCC(N[[email protected]@H](C(C)(C)C)C(N1C[[email protected]](O)C[[email protected]]1C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)=O)=O)C(C=C4)=CC=C4C5=CC6=C(C=C5)N(C(C)=O)[[email protected]@H](C)C[[email protected]]6NC7=CC=C(Cl)C=C7

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

Ethanol : 50 mg/mL (48.23 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9646 mL 4.8231 mL 9.6463 mL
5 mM 0.1929 mL 0.9646 mL 1.9293 mL
10 mM 0.0965 mL 0.4823 mL 0.9646 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (2.41 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (2.41 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (2.41 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

MV4;11 or HL60 cells are incubated with MZP-54 at the desired concentration for 48 h on a clear-bottom 384-well plate. Cells are kept in RPMI medium supplemented with 10% FBS, l-glutamine, penicillin, and streptomycin. Initial cell density is 3 × 105 per mL. Cells are treated with various concentrations of MZP-54 or 0.05% DMSO. After treatment, cell viability is measured with cell viability assay kit. Signal is recorded. Data are analyzed with Graphpad Prism software to obtain EC50 values of each MZP-54[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

MZP-54MZP54MZP 54PROTACEpigenetic Reader DomainProteolysis-targeting chimeraInhibitorinhibitorinhibit

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Product Name:
MZP-54
Cat. No.:
HY-112376
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