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Purity: ≥98%
MZP-54 is a novel, potent and selective PROTAC-based degrader of BRD3/4 with a Kd of 4 nM for Brd4BD2. The design of proteolysis-targeting chimeras (PROTACs) is a powerful small-molecule approach for inducing protein degradation. PROTACs conjugate a target warhead to an E3 ubiquitin ligase ligand via a linker.
| ln Vitro |
Based on PROTAC technology, MZP-54 is a BRD3/4 selective degrader with a Kd of 4 nM for Brd4BD2. With a Kd of 105 ± 24 nM, MZP-54 binds to the VHL-EloC-EloB protein (VCB). With pEC50 values of 7.08 ± 0.05 for MV4;11 and 6.37 ± 0.03 for HL60 cells, MZP-54 exhibits inhibitory effect against these two cell types. MZP-54 displays elevated amounts of cMyc as well [1].
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| References |
[1]. Chan KH, et al. Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J Me
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| Molecular Formula |
C55H66CLN7O9S
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| Molecular Weight |
1036.67205190659
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| CAS # |
2010159-47-2
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| 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
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| Synonyms |
MZP-54; MZP 54; MZP54
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
Ethanol : ~50 mg/mL (~48.23 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.41 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.41 mM) (saturation unknown) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.41 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Chemical Structures of VHL-Targeting PROTACs Based on4and3Used in This Study and Chemical Structure of CRBN-Targeting PROTAC11(ARV-825).
Antiproliferative and Myc-suppression activity of BET degraders and inhibitors: J Med Chem.2018Jan 25;61(2):504-513. |
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 Co-crystal structures to guide PROTAC linking design. First bromodomain of Brd4 with bound (a)3(green carbons, PDB code 3MXF) and (b)4(cyan carbons, PDB code 4BJX). Arrows highlight exit vectors for linking.
PROTACs’ SAR correlation plots. |
 Protein degradation profile of VHL-based BET degraders. HeLa cells were treated for 24 h. Protein levels are shown from one representative of two biological replicates, visualized by immunoblot (a, c) and quantified relative to DMSO control (b, d).
Measuring cooperativities of ternary complex formation by ITC: (a) VCB titrated into10alone; (b) VCB titrated into Brd4BD2–10binary complex; (c) VCB titrated into Brd2BD1–10.
J Med Chem.2018Jan 25;61(2):504-513 |
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