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(+)-JQ1 bump, acid functionalized

Cat. No. 7689 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： Functionalized BET bromodomain ligand; precursor for Tag Degraders
化学名： (R)-2-((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)butanoic acid
纯度： ≥98% (HPLC)
说明书
引用文献
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文献 (3)
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 (+)-JQ1 bump, acid functionalized

(+)-JQ1 bump, acid functionalized is a BET bromodomain binding analog of (+)-JQ1 (Cat. No. 4499) that selectively binds single point mutant form of Brd4 (Brd4BD2 L387A). Functionalized with a carboxylic acid group to enable onward chemistry. The position of the carboxylic acid group represents an 'exit vector' allowing modification without interfering with compound binding ability.

技术数据 for (+)-JQ1 bump, acid functionalized

分子量 428.94
公式 C21H21ClN4O2S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2421153-77-5
InChI Key UAFUXHFSKWIFOW-QAPCUYQASA-N
Smiles CC1=C(C)C(C(C2=CC=C(C=C2)Cl)=N[C@@H]([C@H](C(O)=O)CC)C3=NN=C(C)N43)=C4S1

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 (+)-JQ1 bump, acid functionalized

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 42.89 100

制备储备液 for (+)-JQ1 bump, acid functionalized

以下数据基于产品分子量 428.94。 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 2.33 mL 11.66 mL 23.31 mL
5 mM 0.47 mL 2.33 mL 4.66 mL
10 mM 0.23 mL 1.17 mL 2.33 mL
50 mM 0.05 mL 0.23 mL 0.47 mL

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产品说明书 for (+)-JQ1 bump, acid functionalized

分析证书/产品说明书
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化学品安全技术说明书

参考文献 for (+)-JQ1 bump, acid functionalized

参考文献是支持产品生物活性的出版物。

Bond et al (2021) Development of BromoTag: a 'Bump-and-Hole'-PROTAC system to induce potent, rapid, and selective degradation of tagged target proteins. J.Med.Chem 64 15477 PMID: 34652918

If you know of a relevant reference for (+)-JQ1 bump, acid functionalized, please let us know.

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该领域的文献

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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
Developing Degraders Poster

Developing Degraders Poster

This poster describes the generation of a database of Degraders (PROTACs®) from the literature. The Degraders were profiled according to the constituent ligands, linker type, linker length and physicochemical properties and this information was used to establish a set of guidelines for the design and synthesis of cell-permeable Degrader molecules. Presented at the 20th SCI/RSC Medicinal Chemistry Symposium 2019, Cambridge, UK.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

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