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.

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.

All Tocris products are intended for laboratory research use only.

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 solvent 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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Safety Datasheet

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, Hypoxia, Inducible, Factors, PROTACs, 6154, Tocris Bioscience

Citations for MZ 1

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Literature in this Area

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