NR 7h

Catalog # Availability Size / Price Qty
7177/5
NR 7h | Active Degraders
1 Image
Description: Potent and selective p38α and p38β degrader; 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%

Product Details
Reviews

Biological Activity

Potent and selective p38α and p38β degrader (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. Active in vivo.

Technical Data

M.Wt:
998.87
Formula:
C48H50BrF2N9O8
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥97%
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.

Additional Information

Licensing Caveats:
Sold with kind permission of IRB Barcelona.

Background References

  1. Optimal linker length for small molecule PROTACs that selectively target p38α and p38β for degradation.
    Donoghue et al.
    Cell Chem.Bio., 2019;

Product Datasheets

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