Catalog No.: PC-43049Not For Human Use, Lab Use Only.
Decernotinib (VX-509, VRT-831509) is a potent, selective, orally available JAK3 inhibitor with Ki of 2.5 nM and cellular IC50 of 50-170 nM, demonstrates limited inhibition of JAK1/JAK2/TYK2 in cell-based assays (25-100 fold).
Decernotinib (VX-509, VRT-831509) is a potent, selective, orally available JAK3 inhibitor with Ki of 2.5 nM and cellular IC50 of 50-170 nM, demonstrates limited inhibition of JAK1/JAK2/TYK2 in cell-based assays (25-100 fold).
Decernotinib also inhibits JAK1, JAK2 and TYK2 (Ki=11, 13 and 11 nM) in biochemical assay and shows >400-fold selectivity over a broad kinases.
Decernotinib inhibits IL-2–induced STAT-5 phosphorylation in IL-2–dependent T-cell line with IC50 of 99 nM, potently suppresses T-cell proliferation with IC50 of 170 nM.
Decernotinib modulates proinflammatory response in models of immune-mediated diseases, such as collagen-induced arthritis and delayed-type hypersensitivity.
