HG-9-91-01 is an inhibitor of salt-inducible kinases (SIKs; IC50s = 0.92, 6.6, and 9.6 nM for SIK1, SIK2, and SIK3, respectively). It also inhibits Src, Lck, Yes, and BTK, as well as FGF and Ephrin receptors. HG-9-91-01 increases LPS-stimulated IL-10 production and suppresses pro-inflammatory cytokine secretion in bone marrow-derived macrophages. SIK inhibitors, including HG-9-91-01, enhance CREB-dependent gene transcription and IL-10 production in bone marrow-derived dendritic cells, THP-1 cells, and human primary macrophages.
