An inhibitor of RIPK2 (IC50 = 130 nM in a kinase assay using human recombinant RIPK2); selective for RIPK2 over RIPK1, 4, and 5 (Kds = 46, >10,000, >10,000, and >10,000 nM, respectively) and a panel of 95 kinases at a concentration of 1 μM; reduces levels of RIPK2 phosphorylation at Ser176 in MDP-stimulated BMDMs; decreases MDP-induced transcription of TNF and IL-6 in BMDMs and reduces mRNA levels of the NF-κB target genes TNF, IL-8, IL-1β, and A20 in MDP-stimulated THP-1 cells in a concentration-dependent manner; reduces plasma levels of TNF and delays disease onset in a mouse model of EAE when administered at doses ranging from 3-10 mg/kg
Size
25 mg
Concentration
n/a
Applications
n/a
Other Names
WEHI345 RIPK-2 1 ser 176 IL8 IL1β NFκB THP1 A 20 interleukin