Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: N-[2-[4-amino-3-(4-methylphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-2-methylpropyl]-4-pyridinecarboxamide
Purity: ≥98%
Formula Markup: C22H23N7O
Formula Weight: 401.5
CAS Number: 1354825-58-3
Notes: WEHI-345 is an inhibitor of receptor-interacting protein kinase 2 (RIPK2; IC50 = 130 nM in a kinase assay using human recombinant RIPK2).{41305} It is 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. WEHI-345 reduces levels of RIPK2 phosphorylation at Ser176 in bone marrow-derived macrophages (BMDMs) stimulated by muramyl dipeptide (MDP). It 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. WEHI-345 (3-10 mg/kg) reduces plasma levels of TNF and delays disease onset in a mouse model of experimental autoimmune encephalomyelitis (EAE).
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