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NR 7h

Cat. No. 7177 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 p38α and p38β Degrader (PROTAC®); active in vivo
化学名： 3-(3-Bromo-4-((2,4-difluorobenzyl)oxy)-6-methyl-2-oxopyridin-1(2H)-yl)-N-(4-(1-(4-((4-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)butyl)amino)-4-oxobutyl)-1H-1,2,3-triazol-4-yl)butyl)-4-methylbenzamide
纯度： ≥97% (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 NR 7h

NR 7h is a potent and selective p38α and p38β Degrader (PROTAC®) (DC50 < 50 nM). Displays no significant degradation of p38γ, p38δ, JNK1/2 or ERK1/2. Inhibits phosphorylation of MK2 in UV-treated cancer cells and LPS-stimulated bone marrow-derived macrophages (BMDM). Exhibits similar effect to p38α gene knockout in BBL358 cells. NR 7h impairs replication of Mayaro virus in human dermal fibroblasts and HeLa cells. Active in vivo.

p38α antibody validated for Simple Western™ (automated Western) instruments also available: Catalog # AF8691.

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

许可信息

Sold with kind permission of IRB Barcelona.

技术数据 for NR 7h

E3 ligase CRBN
DC50 24 nM (p38α), 48 nM (p38β) - Degradation in T47D/MB-MDA-231 cells after 24 h treatment
Selectivity confirmed by global proteomics Yes
分子量 998.87
公式 C48H50BrF2N9O8
储存 Store at -20°C
纯度 ≥97% (HPLC)
CAS Number 2550399-06-7
InChI Key BEMLUUUHZPFCBS-UHFFFAOYSA-N
Smiles FC1=CC(F)=C(COC2=C(Br)C(N(C3=C(C)C=CC(C(NCCCCC4=CN(CCCC(NCCCCNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)=O)N=N4)=O)=C3)C(C)=C2)=O)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 NR 7h

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 99.89 100

制备储备液 for NR 7h

以下数据基于产品分子量 998.87。 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 5.01 mL 10.01 mL
5 mM 0.2 mL 1 mL 2 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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参考文献 for NR 7h

参考文献是支持产品生物活性的出版物。

Donoghue et al (2020) Optimal linker length for small molecule PROTACs that selectively target p38α and p38β for degradation. Eur.J.Med.Chem. 201 112451 PMID: 32634680

Sugasti-Salazar et al (2021) Inhibition of p38 mitogen-activated protein kinase impairs mayaro virus replication in human dermal fibroblasts and HeLa cells. Viruses 13 1156 PMID: 34204188

If you know of a relevant reference for NR 7h, please let us know.

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关键词: NR 7h, NR 7h supplier, NR7h, protac, PROTACs, p38alpha, alfa, p38a, α, p38beta, p38b, β, MAPK, Proteolysis, targeted, chimeras, in, vivo, active, degraders, degrades, protein, degradation, tpd, p38, Other, Antivirals, Mitogen, Activated, Protein, Kinase, (MAPK), Degraders, 7177, 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!

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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