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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.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Sold with kind permission of IRB Barcelona.
Technical Data for NR 7h
|Storage||Store at -20°C|
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|
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 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|
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
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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Epigenetics Scientific Review
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Epigenetics in Cancer Poster
Adapted from the 2015 Cancer Product Guide Edition 3, 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
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