BMS 986165

BMS 986165

CAT N°: 33524
Price:

66.00 56.10

BMS 986165 is an allosteric inhibitor of tyrosine kinase 2 (TYK2; IC50 = 0.2 nM for the recombinant TYK2 pseudokinase domain).{62105} 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-?-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-? 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-? 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.

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