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NR 7h

Catalog #: 7177 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
7177/5

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NR 7h | CAS No. 2550399-06-7 | Active Degraders
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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%

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Biological Activity

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.

Technical Data

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
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥97%
Storage:
Store at -20°C
CAS No:
2550399-06-7

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.

Additional Information

Licensing Caveats:
Sold with kind permission of IRB Barcelona.

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