Chemical Name: (-)-3-[3-Bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxo-1(2H)-pyridinyl]-N,4-dimethylbenzamide
Biological ActivityPotent and selective p38α/β inhibitor (IC50 values are 26 and 102 nM, respectively). Exhibits >100-fold selectivity for p38α/β over 71 other kinases, enzymes and GPCRs, including p38γ, p38δ, JNK and ERK2. Inhibits LPS-induced TNFα production in U937 monocytes in vitro. Suppresses acute and chronic inflammatory responses in rat models of arthritis. Orally active.
PH 797804 is the (-)-atropisomer, which is 100-fold more potent than its (+)-atropisomer.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
- PH 797804 is the (-)-atropisomer, which is 100-fold more potent than its (+)-atropisomer
Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation.
Hope et al.
Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase.
Selness et al.
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