RO9021 is an orally bioavailable, ATP-competitive, highly selective inhibitor of Syk kinase with IC50 of 5.6 nM.
RO9021 suppresses BCR signaling in hPBMC and FcγR signaling in human monocytes.
RO9021 blocks osteoclastogenesis from mouse bone marrow macrophages in vitro, also inhibits TLR9 signaling in human Bcells.
RO9021 also potently inhibits type I interferon production by human plasmacytoid dendritic cells (pDC) upon TLR9 activation, inhibits arthritis progression in the mCIA model.
