Poseltinib

Poseltinib (HM71224) is an orally active, selective, irreversible small molecule Bruton tyrosine kinase (BTK) inhibitor. With an IC₅₀ of 1.95 nM. Poseltinib effectively inhibits the signaling mediated by B cell receptors (BCR), Fc receptors (FcR), and Toll-like receptors (TLR). Poseltinib has anti-inflammatory activity and can be used in the research of rheumatoid arthritis^[1][2][3]. IC50 & Target:IC50: 1.95 nM (BTK)^[1] In Vitro:Poseltinib (0.1-100 nM, 30 min) inhibits BCR and FcR signaling in B cells^[1].
Poseltinib (1-1000 nM, 1 h) inhibits the phosphorylation of Btk and its downstream molecules such as PLCγ2, in activated Ramos B lymphoma cells in a dose-dependent manner.
Inhibits the production of tumor necrosis factor (TNF)-α, interleukin (IL)-6, and IL-1β by human monocytes, and osteoclast formation by human monocytes in primary human B cells ^[2].
[3].
In Vivo:Poseltinib (3,-30 mg/kg, p.o, once a day, from 18 to 40 weeks) reduces the overactivity of B cells by inhibiting BTK, alleviating the development of systemic lupus erythematosus (SLE) and lupus nephritis (LN)^[1].
Poseltinib (1-30 mg/kg p.o, once a day for 2 weeks) improves experimental arthritis in mice ^[2].