NR 7h

Name: NR 7h
Brand: Tocris Bioscience
SKU: 7177

Tocris Bioscience, part of Bio-Techne | Catalog # 7177

COA / SDS

Potent and selective p38α and p38β Degrader (PROTAC®); active in vivo

Key Product Details

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)
Molecular Weight:	998.87

View Full Technical Details for NR 7h

Technical Data
Citations

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

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
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

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 for NR 7h

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.00 mL	5.01 mL	10.01 mL
5 mM	0.20 mL	1.00 mL	2.00 mL
10 mM	0.10 mL	0.50 mL	1.00 mL
50 mM	0.02 mL	0.10 mL	0.20 mL

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References for NR 7h

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

Sugasti-Salazar Inhibition of p38 mitogen-activated protein kinase impairs mayaro virus replication in human dermal fibroblasts and HeLa cells. Viruses 2021 PMID: 34204188
Donoghue Optimal linker length for small molecule PROTACs that selectively target p38α and p38β for degradation. Eur.J.Med.Chem. 2020 PMID: 32634680