In vitro
As an ATP competitive kinase inhibitor, INCB028050 (Baricitinib, LY3009104) was a potent inhibitor of JAK1 and JAK2 with IC50 values of 5.9 and 5.7 nM, respectively. INCB0-28050 (Baricitinib, LY3009104), a potent and selective inhibitor of JAK1/2, is shown to inhibit signaling from pathogenic cytokines such as IL-6 and IL-23. Inhibition of JAK signaling prevents the production of chemokines and cytokines associated with uncontrolled RA. In cell-based assays, INCB028050 proved to be a potent inhibitor of JAK signaling and function. In PBMCs, 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 isolated naive T-cells, INCB028050 also inhibited pSTAT3 stimulated by IL-23 (IC 50 = 20 nM).
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