MZ 1

Name: MZ 1
Brand: Tocris Bioscience
SKU: 6154

Tocris Bioscience, part of Bio-Techne | Catalog # 6154

Citations (17)

COA / SDS

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

Key Product 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)
Molecular Weight:	1002.64

View Full Technical Details for MZ 1

Technical Data
Citations

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 (K_d = 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.

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.

Scientific Data Examples for MZ 1

	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.

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
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 for MZ 1

	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 will affect the solvent volumes required to prepare stock solutions.

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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References for MZ 1

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

Zhou A comprehensive review of BET-targeting PROTACs for cancer therapy. Bioorg.Med.Chem. 2022 PMID: 36202064
Gadd Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat.Chem.Biol. 2017 PMID: 28288108
Wurz A " click chemistry platform" for the rapid synthesis of bispecific molecules for inducing protein degradation. J.Med.Chem. 2017 PMID: 28378579
Zengerle Selective small molecule induced degradation of the BET bromodomain protein BRD4. ACS.Chem.Biol 2015 PMID: 26035625