MZ 1

Name: MZ 1
Brand: MedChemExpress
SKU: HY-107425
Rating: 5.0 (24 reviews)

Cat. No.: HY-107425 Pureza: 99.86%: Ficha de datos
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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.

No. CAS : 1797406-69-9

Tamaño	Stock	Cantidad
1 mg	En stock	Estimated Time of Arrival: December 31
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtener un presupuesto
500 mg	Obtener un presupuesto

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Revisión del cliente

Based on 24 publication(s) in Google Scholar

Other Forms of MZ 1:

cis-MZ 1 In-stock
cis-MZ 1 hydrate Obtener un presupuesto
MZ 1 (Standard) Obtener un presupuesto

24 Publications Citing Use of MCE MZ 1

Cell Proliferation/Viability Assay

RT-PCR

Flow Cytometry

: 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.

: 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).

: 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).

: 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.

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Ver todos los productos específicos de isoformas PROTACs:

Ver todas las isoformas

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

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].

Cellular Effect

Cell Line	Type	Value	Description	References
EOL1	IC₅₀	1.5 1 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]
EOL1	IC₅₀	1.5 1 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]
HL-60	IC₅₀	1.5 1 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 1 Compound: 25; MZ1	Antiproliferative activity against human MV4-11 cells Antiproliferative activity against human MV4-11 cells	[PMID: 35763424]
HL-60	IC₅₀	1.5 1 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]
HeLa	DC₅₀	< 100 1 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]
MV4-11	IC₅₀	11.3 1 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.

Peso molecular

1002.64

Fòrmula

C₄₉H₆₀ClN₉O₈S₂

No. CAS

1797406-69-9

Appearance

Solid

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)

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)

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

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, 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
Calculadora de dilución

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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% 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.
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% 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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureza y Documentación

Purity: 99.86%

Select Batch:

Ficha de datos (272 KB) SDS (643 KB)

COA (244 KB) HNMR (157 KB) RP-HPLC (162 KB) LCMS (234 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]

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

MZ 1 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.

Keywords:

MZ 11797406-69-9MZ1MZ-1PROTACsEpigenetic Reader DomainselectiveproteindegradationBRD4DegraderLS174tcellsInhibitorinhibitorinhibit

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MZ 1

Revisión del cliente

Other Forms of MZ 1:

MZ 1 Related Antibodies

24 Publications Citing Use of MCE MZ 1

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas PROTACs:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

MZ 1 Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

MZ 1 Related Classifications

Keywords:

Productos vistos recientemente:

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