Baricitinib (LY3009104, INCB028050) is a potent, selective and orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9/5.7 nM, respectively.
Baricitinib (LY3009104, INCB028050) shows moderate selectivity against Tyk2 (IC50=53 nM) and 100-fold selectivity over JAK3.
INCB028050 inhibited IL-6–stimulated phosphorylation of the canonical substrate STAT3 (pSTAT3) and subsequent production of the chemokine MCP-1 with IC50 values of 44 nM and 40 nM, respectively, in PBMCs.
Baricitinib (LY3009104, INCB028050) suppressed phosphorylated STAT3 in the peripheral blood of rAIA animals.
Baricitinib (LY3009104, INCB028050) (10 mg/kg) reduces elevated cytokine mRNA levels in draining lymph nodes from rats with AIA.
