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生物活性 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) also available.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Sold under licence from the University of Dundee.
技术数据 for VZ 185
|储存||Store at -20°C|
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for VZ 185
|溶剂||最高浓度 mg/mL||最高浓度 mM|
制备储备液 for VZ 185
以下数据基于产品分子量 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.
|浓度/溶剂体积/质量||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|
参考文献 for VZ 185
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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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
Targeted Protein Degradation Research Product GuideUpdated
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Custom Degrader Services
- Ubiquitin-Proteasome System Proteins and Assays
- Assays for Protein Degradation
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics in Cancer Poster
Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
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