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Description: Potent and selective BRD7/9 Degrader (PROTAC®)
Chemical Name: (2S,4R)-N-(2-((5-(4-(2,6-Dimethoxy-4-(2-methyl-1-oxo-1,2-dihydro-2,7-naphthyridin-4-yl)benzyl)piperazin-1-yl)pentyl)oxy)-4-(4-methylthiazol-5-yl)benzyl)-1-((S)-2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Biological Activity for VZ 185
VZ 185 is a potent and selective VHL-based dual Degrader (PROTAC®) of BRD7/9 (DC50 values are 4 and 34 nM for BRD7 and BRD9, respectively). Exhibits selectivity for BRD7/9 degradation over other bromodomain-containing proteins and other BAF/PBAF subunits. Displays cytotoxicity towards EOL-1 and A-204 cancer cell lines.
Negative control cis VZ 185 (Cat. No. 6939) and BRD7 antibody validated for Western Blot also available: Catalog # NBP1-28727.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Licensing Information
Sold under licence from the University of Dundee.
Technical Data for VZ 185
| E3 ligase | VHL |
| DC50 / Dmax | 4.5 nM / 95% (BRD7), 1.79 nM / 95% (BRD9) - Degradation in RI-1 cells after 8 h treatment |
| Selectivity confirmed by global proteomics | Yes |
| M. Wt | 995.23 |
| Formula | C53H67FN8O8S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2306193-61-1 |
| PubChem ID | 138454768 |
| InChI Key | ZAGCLFXBHOXXEN-JPTLTNPLSA-N |
| Smiles | CN(C(C1=C2C=CN=C1)=O)C=C2C3=CC(OC)=C(C(OC)=C3)CN4CCN(CC4)CCCCCOC5=CC(C6=C(N=CS6)C)=CC=C5CNC([C@@H]7C[C@H](CN7C([C@H](C(C)(C)C)NC(C8(CC8)F)=O)=O)O)=O |
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 for VZ 185
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 99.52 | 100 |
Preparing Stock Solutions for VZ 185
The following data is based on the product molecular weight 995.23. 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 | 5.02 mL | 10.05 mL |
| 5 mM | 0.2 mL | 1 mL | 2.01 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 for VZ 185
References for VZ 185
References are publications that support the biological activity of the product.
Zoppi et al (2019) Iterative design and optimization of initially inactive Proteolysis Targeting Chimeras (PROTACs) identify VZ185 as a potent, fast, and selective von Hippel-Lindau (VHL) based dual degrader probe of BRD9 and BRD7. J.Med.Chem. 62 699 PMID: 30540463
Riching et al (2021) Translating PROTAC chemical series optimization into functional outcomes underlying BRD7 and BRD9 protein degradation. Curr.Res.Chem.Biol. 1 100009
If you know of a relevant reference for VZ 185, please let us know.
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Keywords: VZ 185, VZ 185 supplier, VZ185, potent, selective, VHL, active, degraders, degrades, PROTACs, protac, BRD7, BRD9, targeted, protein, degradation, tpd, Bromodomains, Bromodomain, (BRD), Degraders, 6936, Tocris Bioscience
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TPD and Induced Proximity Research Product GuideUpdated
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Assays for Protein Degradation
- Induced Proximity Tools
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. Presented at EFMC 2018, Ljubljana, Slovenia