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VZ 185

Cat. No. 6936 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent and selective BRD7/9 Degrader (PROTAC®)
化学名： (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
纯度： ≥98% (HPLC)
说明书
引用文献
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文献 (2)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

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) 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.

许可信息

Sold under licence from the University of Dundee.

技术数据 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
分子量 995.23
公式 C53H67FN8O8S
储存 Store at -20°C
纯度 ≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

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
溶解性
DMSO 99.52 100

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.

选择批次从而根据批次分子量重新计算:
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

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产品说明书 for VZ 185

分析证书/产品说明书
选择另一批次：
化学品安全技术说明书

参考文献 for VZ 185

参考文献是支持产品生物活性的出版物。

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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关键词: 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 Guide

TPD and Induced Proximity Research Product Guide

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

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