WEHI-345

WEHI-345

CAT N°: 23023
Price:

From 85.00 72.25

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 ?M. 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-?B target genes TNF, IL-8, IL-1?, 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).

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • N-[2-[4-amino-3-(4-methylphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-2-methylpropyl]-4-pyridinecarboxamide
  • Correlated keywords
    • WEHI345 RIPK-2 1 ser 176 IL8 IL1? NF?B THP1 A 20 interleukin
  • Product Overview:
    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 ?M. 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-?B target genes TNF, IL-8, IL-1?, 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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