WEHI-345

WEHI-345 is an inhibitor of receptor-interacting protein kinase 2 (RIPK2, IC50 = 130 nM in a kinase assay using human recombinant RIPK2). 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-kappaB target genes TNF, IL-8, IL-1beta, 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).Formal Name: N-[2-[4-amino-3-(4-methylphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-2-methylpropyl]-4-pyridinecarboxamide. CAS Number: 1354825-58-3. Molecular Formula: C22H23N7O. Formula Weight: 401.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMSO: 2 mg/ml, Ethanol: slightly soluble. lambdamax: 252 nm. SMILES: CC(C=C1)=CC=C1C2=NN(C(C)(C)CNC(C3=CC=NC=C3)=O)C4=NC=NC(N)=C42. InChi Code: InChI=1S/C22H23N7O/c1-14-4-6-15(7-5-14)18-17-19(23)26-13-27-20(17)29(28-18)22(2,3)12-25-21(30)16-8-10-24-11-9-16/h4-11,13H,12H2,1-3H3,(H,25,30)(H2,23,26,27). InChi Key: LEBSTCDZKUSVOY-UHFFFAOYSA-N.