AMG-548 hydrochloride is a selective, orally active p38alpha inhibitor with a Ki value of 0.5 nM, a slight selectivity for p38beta (Ki=36 nM) and a 1000-fold selectivity for p38gamma and p38delta. AMG 548 hydrochloride also effectively inhibits whole blood LPS-stimulated TNFalpha with an IC50 value of 3 nM. AMG-548 hydrochloride directly inhibited casein kinase 1 isoforms delta and epsilon, which in turn inhibited Wnt signaling.
Molekulargewicht:
498.02
Formel:
C29H28ClN5O
Target-Kategorie:
Others|||Casein Kinase|||p38 MAPK
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