NR 7h
Tocris Bioscience, part of Bio-Techne | Catalog # 7177
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
Product Description
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.Product Specifications
Molecular Weight
998.87
Formula
C48H50BrF2N9O8
Storage
Store at -20°C
Purity
≥97% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for NR 7h
For research use only
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