Description
Decernotinib (VX-509, VRT-831509) is a potent, selective, orally available JAK3 inhibitor with Ki of 2.5nM and cellular IC50 of 50-170nM, demonstrates limited inhibition of JAK1/JAK2/TYK2 in cell-based assays (25-100 fold); also inhibits JAK1, JAK2 and TYK2 (Ki=11, 13 and 11nM) in biochemical assay and shows >400-fold selectivity over a broad kinases; inhibits IL-2-induced STAT-5 phosphorylation in IL-2-dependent T-cell line with IC50 of 99nM, potently suppresses T-cell proliferation with IC50 of 170nM; modulates proinflammatory response in models of immune-mediated diseases, such as collagen-induced arthritis and delayed-type hypersensitivity. Rheumatoid Arthritis Phase 2 Discontinued