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

MZP-54 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, with a Kd of 4 nM for Brd4BD2.

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MZP-54 Chemical Structure

MZP-54 Chemical Structure

CAS No. : 2010159-47-2

Size Price Stock Quantity
Solution
10 mM * 1 mL in Ethanol USD 605 In-stock
Solid
5 mg USD 550 In-stock
10 mg USD 850 In-stock
25 mg USD 1600 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

MZP-54 is a PROTAC connected by ligands for von Hippel-Lindau and BRD3/4, 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].

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

Molecular Weight

1036.67

Formula

C55H66ClN7O9S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N1C[C@H](O)C[C@H]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)[C@@H](C)C[C@H]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 2 years
-20°C 1 year
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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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% EtOH    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.41 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 EtOH 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% EtOH    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.41 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 EtOH 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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol 1 mM 0.9646 mL 4.8231 mL 9.6463 mL 24.1157 mL
5 mM 0.1929 mL 0.9646 mL 1.9293 mL 4.8231 mL
10 mM 0.0965 mL 0.4823 mL 0.9646 mL 2.4116 mL
15 mM 0.0643 mL 0.3215 mL 0.6431 mL 1.6077 mL
20 mM 0.0482 mL 0.2412 mL 0.4823 mL 1.2058 mL
25 mM 0.0386 mL 0.1929 mL 0.3859 mL 0.9646 mL
30 mM 0.0322 mL 0.1608 mL 0.3215 mL 0.8039 mL
40 mM 0.0241 mL 0.1206 mL 0.2412 mL 0.6029 mL
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MZP-54 Related Classifications

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.

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MZP-54
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