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NR 7h

Cat. No. 7177 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

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
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

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
Solubility
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.

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Citations for NR 7h

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Literature in this Area

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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