NR 7h

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Description: Potent and selective p38α and p38β Degrader (PROTAC®); active in vivo
Chemical Name: 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
Purity: ≥97% (HPLC)
Literature (4)

Biological Activity 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.

Licensing Information

Sold with kind permission of IRB Barcelona.

Technical Data 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
M. Wt 998.87
Formula C48H50BrF2N9O8
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 2550399-06-7
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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for NR 7h

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 99.89 100

Preparing Stock Solutions for NR 7h

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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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References for NR 7h

References are publications that support the biological activity of the product.

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.

Keywords: 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, Protein, Degraders, p38, Other, Antivirals, 7177, Tocris Bioscience

Citations for NR 7h

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Literature in this Area

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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Targeted Protein Degradation Research Product Guide

Targeted Protein Degradation Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
Epigenetics Scientific Review

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics in Cancer Poster

Epigenetics in Cancer Poster

This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

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