MZ 1
Tocris Bioscience, part of Bio-Techne | Catalog # 6154
(+)-JQ1 based Degrader (PROTAC®) that preferentially degrades BRD4
Key Product Details
Description
(+)-JQ1 based Degrader (PROTAC®) that preferentially degrades BRD4
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.
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 DundeeExternal 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
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.
| 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for MZ 1
For research use only
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