Referencia número: HY-107425

MZ 1

25 Cited Publications

Revisión del cliente

Based on 25 publication(s) in Google Scholar

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. K_ds 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)).

Para uso exclusivo en investigación. No vendemos a pacientes.

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.

Pureza: 99.86%
No. CAS: 1797406-69-9
Fòrmula: C₄₉H₆₀ClN₉O₈S₂
Peso molecular:1002.64

Almacenamiento:

-20°C, stored under nitrogen

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

MZ 1 Chemical Structure

No. CAS: 1797406-69-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (25)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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. K_ds 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].

Ver todos los productos específicos de isoformas PROTACs :

Ver todos los productos específicos de isoformas Epigenetic Reader Domain :

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]

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].

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

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.

Chemical Information

No. CAS 1797406-69-9
Appearance Solid
Peso molecular 1002.64
Fòrmula C₄₉H₆₀ClN₉O₈S₂
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

-20°C, stored under nitrogen

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

Publications (25)

All Cell Proliferation/Viability AssayRT-PCRFlow CytometryWB

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Journal Impact Factor

Nature

Programming inactive RNA-binding small molecules into bioactive degraders. [Abstract]

2023 Jun;618(7963):169-179. PMID: 37225982

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).
Mol Cell

Cullin-RING ligases employ geometrically optimized catalytic partners for substrate targeting. [Abstract]

2024 Apr 4;84(7):1304-1320.e16. PMID: 38382526
Nat Commun

The ESCRT protein CHMP5 promotes T cell leukemia by enabling BRD4-p300-dependent transcription. [Abstract]

2025 May 3;16(1):4133. PMID: 40319015

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.
Nat Commun

Stromal induction of BRD4 phosphorylation Results in Chromatin Remodeling and BET inhibitor Resistance in Colorectal Cancer. [Abstract]

2021 Jul 21;12(1):4441. PMID: 34290255
Adv Sci (Weinh)

Discovery of SKP2-Recruiting PROTACs for Target Protein Degradation. [Abstract]

2026 Apr;13(20):e15159. PMID: 41637562
Nat Chem Biol

Template-assisted covalent modification underlies activity of covalent molecular glues. [Abstract]

2024 Dec;20(12):1640-1649. PMID: 39075252

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).
Nat Chem Biol

Activity-based profiling of cullin-RING E3 networks by conformation-specific probes. [Abstract]

2023 Dec;19(12):1513-1523. PMID: 37653169
J Adv Res

Redistribution of super-enhancers promotes malignancy in human hepatocellular carcinoma. [Abstract]

2025 Jul 4:S2090-1232(25)00504-1. PMID: 40617410
J Control Release

The HSP90-dependent bioorthogonal PROTAC prodrug system enables tumor-selective and enhanced protein degradation. [Abstract]

2026 May 10:393:114828. PMID: 41839264
Nat Struct Mol Biol

Mechanism of millisecond Lys48-linked poly-ubiquitin chain formation by cullin-RING ligases. [Abstract]

2024 Feb;31(2):378-389. PMID: 38326650
Nat Struct Mol Biol

CAND1 inhibits Cullin-2-RING ubiquitin ligases for enhanced substrate specificity. [Abstract]

2024 Feb;31(2):323-335. PMID: 38177676
NPJ Precis Oncol

Targeting ACE2-BRD4 crosstalk in colorectal cancer and the deregulation of DNA repair and apoptosis. [Abstract]

2023 Feb 18;7(1):20. PMID: 36801948
J Med Chem

Alkyne Two-Phase Strategy: Rapid Generation of TK-285-Derived PROTACs as BRD4 Degraders. [Abstract]

2026 Mar 19. PMID: 41852276
J Med Chem

Peptide Inhibitor Targeting the Extraterminal Domain in BRD4 Potently Suppresses Breast Cancer Both In Vitro and In Vivo. [Abstract]

2024 Apr 25;67(8):6658-6672. PMID: 38569135
Biochem Pharmacol

Discovery of a potent BRD4 PROTAC and evaluation of its bioactivity in breast cancer cell lines. [Abstract]

2025 Jul 12:241:117159. PMID: 40659131
Cancer Biol Ther

BRD4 PROTAC degrader MZ1 exerts anticancer effects in acute myeloid leukemia by targeting c-Myc and ANP32B genes. [Abstract]

2022 Dec 31;23(1):1-15. PMID: 36170346
Structure

PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]

2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
ACS Chem Biol

Cellular Resistance Mechanisms to Targeted Protein Degradation Converge Toward Impairment of the Engaged Ubiquitin Transfer Pathway. [Abstract]

2019 Oct 18;14(10):2215-2223. PMID: 31553577

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.
BMC Cancer

MZ1, a BRD4 inhibitor, exerted its anti-cancer effects by suppressing SDC1 in glioblastoma. [Abstract]

2024 Feb 16;24(1):220. PMID: 38365636
J Immunol

Proteolysis-Targeting Chimeras Enhance T Cell Bispecific Antibody-Driven T Cell Activation and Effector Function through Increased MHC Class I Antigen Presentation in Cancer Cells. [Abstract]

2021 Jul 15;207(2):493-504. PMID: 34215653
Hematology

BRD4 PROTAC degrader MZ1 exhibits anti-B-cell acute lymphoblastic leukemia effects via targeting CCND3. [Abstract]

2023 Dec;28(1):2247253. PMID: 37594294
bioRxiv

Protein Age Bias in Target Degradation by PROTACs. [Abstract]

2026 May 5:2026.05.01.722262. PMID: 42146509
SSRN

2025 Jul 8.
Harvard University

2023 Mar. 30487357.
bioRxiv

Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders. [Abstract]

2023 Feb 15:2023.02.14.528208. PMID: 36824856

Solvente y solubilidad

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (272 KB)
SDS (643 KB)
- English - EN (643 KB)
- Français - FR (643 KB)
- Deutsch - DE (643 KB)
- Norwegian - NO (643 KB)
- Español - ES (643 KB)
- Swedish - SV (643 KB)
- Italian - IT (643 KB)
- Korean - KR (643 KB)
- Portuguese - PT (643 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Zengerle M, et al. Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4. ACS Chem Biol. 2015 Aug 21;10(8):1770-7. [Content Brief]

[2]. Gadd MS, et al. Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat Chem Biol. 2017 May;13(5):514-521. [Content Brief]

[3]. Otto C, et al. Targeting bromodomain-containing protein 4 (BRD4) inhibits MYC expression in colorectal cancer cells. Neoplasia. 2019 Nov;21(11):1110-1120. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

MZ 1

25 Cited Publications

100 mg Obtener un presupuesto

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MZ 1

PROTAC Library

Publications Citing Use of MedChemExpress (MCE) MZ 1

Ver todos los productos específicos de isoformas PROTACs

Ver todos los productos específicos de isoformas Epigenetic Reader Domain

Actividad biológica

Chemical Information

Publications (25)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

MZ 1

PROTAC Library

Publications Citing Use of MedChemExpress (MCE) MZ 1

Ver todos los productos específicos de isoformas PROTACs

Ver todos los productos específicos de isoformas Epigenetic Reader Domain

Actividad biológica

Chemical Information

Publications (25)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

MZ 1 Related Classifications

HY-107425 Related Classifications