(+)-JQ1 maleimide

Pricing Availability   Qty
说明: JQ1-maleimide functionalized probe; induces proteasomal degradation of BRD4
化学名: (S)-N-(2-(2-(2-(2-(4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamido)ethoxy)ethoxy)ethyl)-6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanamide
纯度: ≥95% (HPLC)
说明书
引用文献
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文献 (3)

生物活性 for (+)-JQ1 maleimide

(+)-JQ1 maleimide is a probe that comprises a cysteine-reactive maleimide connected to the BRD4 ligand, JQ1, via a PEG2 linker. It can be used in the COFFEE method (COvalent Functionalization Followed by E3 Electroporation) in which (+)-JQ1 maleimide is covalently attached to VHL followed by electroporation into live cells. The E3 ligase forms a complex with BRD4 intracellularly and induces its degradation.

技术数据 for (+)-JQ1 maleimide

分子量 724.27
公式 C35H42ClN7O6S
储存 Store at -20°C
纯度 ≥95% (HPLC)
InChI Key SGQDAIFBYPRIDQ-MHZLTWQESA-N
Smiles ClC1=CC=C(C2=N[C@@H](CC(NCCOCCOCCNC(CCCCCN3C(C=CC3=O)=O)=O)=O)C4=NN=C(C)N4C5=C2C(C)=C(C)S5)C=C1

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 maleimide

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 72.43 100

制备储备液 for (+)-JQ1 maleimide

以下数据基于产品分子量 724.27。 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 1.38 mL 6.9 mL 13.81 mL
5 mM 0.28 mL 1.38 mL 2.76 mL
10 mM 0.14 mL 0.69 mL 1.38 mL
50 mM 0.03 mL 0.14 mL 0.28 mL

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产品说明书 for (+)-JQ1 maleimide

参考文献 for (+)-JQ1 maleimide

参考文献是支持产品生物活性的出版物。

Pinch et al (2022) A strategy to assess the cellular activity of E3 ligase components against neo-substrates using electrophilic probes. Cell Chem.Biol. 29 57 PMID: 34499862


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

关键词: (+)-JQ1 maleimide, (+)-JQ1 maleimide supplier, TPD, targeted, protein, degradation, maleimide, probe, 2-PEG, linker, COFFEE, COvalent, Functionalization, Followed, E3, Electroporation, BRD4, VHL, Degraders, degrades, Functionalized, Warhead, Ligands, Bromodomains, 7576, Tocris Bioscience

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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