MZ 1

Pricing Availability   Qty

Save up to 40% on RUO Reagents with BIOSPRING24 (see details)

Description: (+)-JQ1 based Degrader (PROTAC®) that preferentially degrades BRD4
Chemical Name: (2S,4R)-1-((S)-2-(tert-butyl)-17-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,16-dioxo-6,9,12-trioxa-3,15-diazaheptadecanoyl)- 4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Citations (8)
Literature (4)

Biological Activity for MZ 1

MZ 1 is a cell penetrant Degrader (PROTAC®) based on (+)-JQ1 (Cat.No. 4499) conjugated to a von Hippel-Lindau (VHL) ligand. MZ 1 induces preferential degradation of BRD4 over BRD2 and BRD3 (DC50 values for degradation of BRD4 are 8 and 23 nM in H661 and H838 cells, respectively), while retaining high affinity for BRD2, BRD3 and BRD4 bromodomains (Kd = 13-60 nM). MZ 1 induces complete degradation of BRD4 at a concentration of 100 nM, whereas complete degradation of BRD2/3 is achieved at 2 μM. Potent cytotoxicity and antiproliferative effects are exhibited in AML cell lines (pEC50 = 7.6 in Mv4-11 cells).

Negative control cis MZ 1 also available.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Scientific Data

Western Blot Application of MZ 1 in HeLa Cells View Larger

Application of MZ 1 in HeLa Cells. Western Blot data showing knockdown of BRD4 long isoform after MZ-1 (Catalog # 6154, 1 μM) treatment of HeLa cells. Protein quantification (relative to DMSO-only control) is shown beneath the corresponding lane. BRD4 antibody is CST#13440 used at 1:2000 dilution. Secondary is Anti-Rabbit HAF008, 1:1000, R&D Systems. GAPDH primary antibody is R&D Systems AF5718 used at 5μg/mL. Secondary is Anti-Goat HAF017, 1:1000, R&D Systems. Data courtesy of Jeff Cooper, Bio-Techne.

Licensing Information

Sold under licence from the University of Dundee

External Portal Information for MZ 1 is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of MZ 1 is reviewed on the Chemical Probes website.

Technical Data for MZ 1

M. Wt 1002.64
Formula C49H60ClN9O8S2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1797406-69-9
PubChem ID 122201421
Smiles CC1=C(C2=C(N3C(C)=NN=C3[C@@H](N=C2C4=CC=C(C=C4)Cl)CC(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5C[C@@H](C[C@H]5C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)O)=O)=O)=O)S1)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for MZ 1

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 100.26 100
ethanol 100.26 100

Preparing Stock Solutions for MZ 1

The following data is based on the product molecular weight 1002.64. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1 mL 4.99 mL 9.97 mL
5 mM 0.2 mL 1 mL 1.99 mL
10 mM 0.1 mL 0.5 mL 1 mL
50 mM 0.02 mL 0.1 mL 0.2 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.


Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Product Datasheets for MZ 1

Certificate of Analysis / Product Datasheet
Select another batch:

References for MZ 1

References are publications that support the biological activity of the product.

Zengerle et al (2015) Selective small molecule induced degradation of the BET bromodomain protein BRD4. ACS.Chem.Biol 10 1770 PMID: 26035625

Gadd et al (2017) Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat.Chem.Biol. PMID: 28288108

Wurz et al (2017) A " click chemistry platform" for the rapid synthesis of bispecific molecules for inducing protein degradation. J.Med.Chem. PMID: 28378579

Zhou et al (2022) A comprehensive review of BET-targeting PROTACs for cancer therapy. Bioorg.Med.Chem. 73 117033 PMID: 36202064

If you know of a relevant reference for MZ 1, please let us know.

Keywords: MZ 1, MZ 1 supplier, MZ1, PROTAC, PROTACs, Proteolysis, targeted, chimeras, Bromodomain, BRD2, BRD3, BRD4, BET, proteins, JQ1, VHL, E3, ubiquitin, ligase, HIF-alpha, HIF-a, HIF-α, active, degraders, degrades, protein, degradation, tpd, Bromodomains, Protein, Degraders, 6154, Tocris Bioscience

8 Citations for MZ 1

Citations are publications that use Tocris products. Selected citations for MZ 1 include:

Ma et al (2023) Engineered PROTAC-CID systems for mammalian inducible gene regulation J Am Chem Soc 145 1593 PMID: 36626587

Philippe et al (2020) Endoplasmic reticulum stress actively suppresses hepatic molecular identity in damaged liver. Mol Syst Biol 16 e9156 PMID: 32407006

Kaji et al (2020) Characterization of cereblon-dependent targeted protein degrader by visualizing the spatiotemporal ternary complex formation in cells. Sci Rep 10 3088 PMID: 32080280

Kristin M et al (2021) Kinetic Detection of E3:PROTAC:Target Ternary Complexes Using NanoBRET Technology in Live Cells. Methods Mol Biol 2365 151-171 PMID: 34432243

Do you know of a great paper that uses MZ 1 from Tocris? Please let us know.

Reviews for MZ 1

There are currently no reviews for this product. Be the first to review MZ 1 and earn rewards!

Have you used MZ 1?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Targeted Protein Degradation Research Product Guide

Targeted Protein Degradation Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
Epigenetics Scientific Review

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics in Cancer Poster

Epigenetics in Cancer Poster

This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia