Cayman BMS 986165

BMS 986165 is an allosteric inhibitor of tyrosine kinase 2 (TYK2; IC₅₀ = 0.2 nM for the recombinant TYK2 pseudokinase domain). It is selective for TYK2 over a panel of 249 protein and lipid kinases at 1 µM but does inhibit the JAK1 pseudokinase domain and bone morphogenetic protein receptor type II (BMPR2; IC₅₀s = 1 and 193 nM, respectively). BMS 986165 inhibits IFN-α-induced phosphorylation of STAT1, -2, -3, and -5 in primary human peripheral blood mononuclear cells (PBMCs; IC₅₀s = 1-6 nM). It also inhibits IL-12-induced production of IFN-γ in human PBMCs (IC₅₀ = 11 nM) and IL-12-induced phosphorylation of STAT4 in NK-92 cells (IC₅₀ = 5 nM). BMS 986165 (1 and 10 mg/kg) reduces IL-12 and IL-18-induced production of IFN-γ in mice. It inhibits IFN-regulated expression of IFIT3, IFIT1, and MX1, genes encoding innate antiviral response proteins, and reduces tubulointerstitial and glomerular nephritis in female NZB/W lupus-prone mice. BMS 986165 also inhibits anti-CD40 antibody-induced colitis and systemic wasting in mice.

WARNING This product is not for human or veterinary use.