Decernotinib is an orally bioavailable Janus kinase 3 (JAK3) inhibitor, potently and selectively inhibiting the enzyme with an in vitro Ki of 2.5 nM, and IC50 of 50-170 nM in cellular assays dependent on JAK3 activity. Highly selective, displaying no activity (with limited or no measureable potency) towards other JAK and non-JAK enzymes. Showed in vivo activity in two animal models of aberrant immune function, and demonstrated dose-dependent reduction in ankle swelling and paw weight and improved paw histopathology scores in the rat collagen-induced arthritis model.

KEYWORDS: Decernotinib | Supplier | JAK3 inhibitor | VX-509 | VRT-831509 | Adelatinib | VX509 | VX 509 | VRT831509 | VRT 831509 | CT-DECE | CAS [944842-54-0] | JAK-STAT Pathway | JAK | Inhibitor | Enzymes