MZ 1

Tocris Bioscience | Catalog # 6154

(+)-JQ1 based Degrader (PROTAC®) that preferentially degrades BRD4
Tocris Bioscience

Key Product Details

Description

(+)-JQ1 based Degrader (PROTAC®) that preferentially degrades BRD4
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Product Description

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 Images for MZ 1

Application of MZ 1 in HeLa Cells

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

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.

Product Specifications for MZ 1

Molecular Weight

1002.64

Formula

C49H60ClN9O8S2

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

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.

Solubility

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
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 all 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 1.00 mL 4.99 mL 9.97 mL
5 mM 0.20 mL 1.00 mL 1.99 mL
10 mM 0.10 mL 0.50 mL 1.00 mL
50 mM 0.02 mL 0.10 mL 0.20 mL

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Background References

References are publications that support the biological activity of the product. See our Citations tab to view 18 publications citing the usage of this product.

Product Documents for MZ 1

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for MZ 1

For research use only

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