MZ 1

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Cat.No. 6154 - MZ 1 | C49H60ClN9O8S2 | CAS No. 1797406-69-9
Description: (+)-JQ1 based PROTAC that selectively degrades BRD4 in cells
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

Cell penetrant Proteolysis Targeting Chimera (PROTAC) compound based on (+)-JQ1 (Cat.No. 4499) conjugated to a von Hippel-Lindau (VHL) ligand. Retains high affinity for BRD2, BRD3 and BRD4 bromodomains (Kd = 13-60 nM) but 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). Exhibits potent cytotoxicity and antiproliferative effects in AML cell lines (pEC50 = 7.6 in Mv4-11 cells). Negative control cis MZ 1 also available.

PROTACs are bi-functional small molecules that harness the ubiquitin/proteasome system (UPS) to selectively and catalytically remove target proteins from cells.

Licensing Information

Sold under licence from the University of Dundee

External Portal Information

Chemicalprobes.org 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.


Application of MZ 1 in HeLa Cells

Application of MZ 1 in HeLa Cells (Cat. No. 6154)



Wes data showing knockdown of BRD4 long isoform after MZ-1 (Cat. No. 6154, 1 μM) treatment of HeLa cells. Protein quantification (relative to DMSO-only control) is shown beneath the corresponding lane.

Data courtesy of Jeff Cooper, Bio-Techne.

Technical Data

M. Wt 1002.64
Formula C49H60ClN9O8S2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1797406-69-9
PubChem ID 122201421
InChI Key PTAMRJLIOCHJMQ-PYNGZGNASA-N
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

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

Preparing Stock Solutions

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.

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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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


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

Keywords: MZ 1, MZ 1 supplier, MZ1, PROTAC, Proteolysis, targeted, chimeras, Bromodomain, BRD2, BRD3, BRD4, BET, proteins, JQ1, VHL, E3, ubiquitin, ligase, HIF-alpha, HIF-a, HIF-α, Ubiquitin, Ligases, Bromodomains, Active, Degraders, 6154, Tocris Bioscience

Citations for MZ 1

Citations are publications that use Tocris products.

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Literature in this Area

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

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

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Targeted Protein Degradation Research Product Guide

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  • Active Degraders (e.g. PROTACs)
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Epigenetics

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

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, 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

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.