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dBET1

Cat. No. 6327 1 次引用 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： (+)-JQ1 based Degrader (PROTAC®) targeting BET bromodomains, active in vivo
化学名： (6S)-4-(4-Chlorophenyl)-N-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
纯度： ≥98% (HPLC)
说明书
引用文献 (1)
评论
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 dBET1

dBET1 is a Degrader (PROTAC®) comprising BET bromodomain antagonist (+)-JQ1 (Cat. No. 4499) conjugated to a cereblon E3 ubiquitin ligase ligand. Depletes BET bromodomains in cancer cell lines in vitro (EC50 = 430 nM in breast cancer cells) and induces apoptosis. Delays tumor growth and downregulates MYC in mice bearing human AML xenografts. Antibody validated for Western Blot also available: NBP2-77359.

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

许可信息

Sold under license from Dana-Farber Cancer Institute.

技术数据 for dBET1

分子量 785.27
公式 C38H37ClN8O7S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1799711-21-9
PubChem ID 91799313
InChI Key LKEGXJXRNBALBV-PMCHYTPCSA-N
Smiles CC1=NN=C2[C@@H](N=C(C3=CC=C(C=C3)Cl)C4=C(N12)SC(C)=C4C)CC(NCCCCNC(COC5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=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 dBET1

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 78.53 100

制备储备液 for dBET1

以下数据基于产品分子量 785.27。 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 1.27 mL 6.37 mL 12.73 mL
5 mM 0.25 mL 1.27 mL 2.55 mL
10 mM 0.13 mL 0.64 mL 1.27 mL
50 mM 0.03 mL 0.13 mL 0.25 mL

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产品说明书 for dBET1

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 dBET1

参考文献是支持产品生物活性的出版物。

Winter et al (2015) Drug Development. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science 348 1376 PMID: 25999370

Wurz et al (2017) A "click chemistry platform" for the rapid synthesis of bispecific molecules for inducing protein degradation. J.Med.Chem. 10.1021 PMID: 28378579

If you know of a relevant reference for dBET1, please let us know.

按标靶查看相关产品

关键词: dBET1, dBET1 supplier, Proteolysis, Targeting, Chimera, PROTAC, PROTACs, cereblon, E3, ubiquitin, ligase, bromodomain, BRD4, targeted, protein, degradation, tpd, active, degraders, degrades, Bromodomains, Bromodomain, (BRD), Degraders, 6327, Tocris Bioscience

1 篇 dBET1 的引用文献

引用文献是使用了 Tocris 产品的出版物。 dBET1 的部分引用包括：

Hao et al (2020) Highly Parallel Quantification and Compartment Localization of Transcription Factors and Nuclear Proteins. Cell Rep 30 2463-2471.e5 PMID: 32101728

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该领域的文献

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。

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