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JQAD1

Cat. No. 7682 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 EP300 Degrader (PROTAC®)
化学名： 12-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)amino)-N-((R)-3'-(2-((4-fluorobenzyl)((S)-1,1,1-trifluoropropan-2-yl)amino)-2-oxoethyl)-2',4'-dioxo-2,3-dihydrospiro[indene-1,5'-oxazolidin]-5-yl)dodecanamide
纯度： ≥98% (HPLC)
说明书
引用文献
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 JQAD1

JQAD1 is a potent and selective histone acetyltransferase EP300 Degrader (PROTAC®; DC50 ≤ 31.6 nM); comprises an EP300 inhibitor, A485 (Cat. No. 6387), joined by a linker to a cereblon E3 ligase ligand. JQAD1 brings about degradation of EP300 in neuroblastoma cell lines in a proteasome-dependent manner. JQAD1 suppresses both H3K27ac and EP300 expression levels and induces apoptosis. JQAD1 suppresses tumor growth in NSG mice xenografted with Kelly cells. CRC and MYCN genes are downregulated in tumors treated with JQAD1. JQAD1 exhibits no significant effect on coactivator CBP at concentrations inducing EP300 degradation.

p300 antibody validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF3789.

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 JQAD1

分子量 932.97
公式 C48H52F4N6O9
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2417097-18-6
PubChem ID 162615894
InChI Key TWCIGBYYSZQAAA-GWWVHQGYSA-N
Smiles C[C@@H](C(F)(F)F)N(C(CN1C(O[C@]2(C1=O)CCC3=CC(NC(CCCCCCCCCCCNC4=CC=C5C(N(C(C5=C4)=O)C6CCC(NC6=O)=O)=O)=O)=CC=C23)=O)=O)CC7=CC=C(C=C7)F

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 JQAD1

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 93.3 100

制备储备液 for JQAD1

以下数据基于产品分子量 932.97。 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 1.07 mL 5.36 mL 10.72 mL
5 mM 0.21 mL 1.07 mL 2.14 mL
10 mM 0.11 mL 0.54 mL 1.07 mL
50 mM 0.02 mL 0.11 mL 0.21 mL

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参考文献 for JQAD1

参考文献是支持产品生物活性的出版物。

Durbin et al (2021) EP300 selectively controls the enhancer landscape of MYCN-amplified neuroblastoma. Cancer Discov. PMID: 34772733

If you know of a relevant reference for JQAD1, please let us know.

按标靶查看相关产品

关键词: JQAD1, JQAD1 supplier, EP300, PROTAC, PROTACs, active, degraders, degrades, histone, acetyltransferase, proteolysis-targeting, chimera, prostate, cancer, potent, selective, Histone, Acetyltransferases, CBP, and, p300, Degraders, 7682, Tocris Bioscience

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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