jak1-jh2

Deucravacitinib is a highly selective, orally bioavailable, allosteric TYK2 inhibitor for the treatment of autoimmune diseases. It blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain, inhibiting IL-12/23 and type I IFN pathways. It selectively binds to the TYK2 pseudokinase (JH2) domain with an IC50 of 1.0 nM.

Tyk2-IN-9 (Compound 26), a selective Tyk-2 inhibitor, exhibits IC50 values of 0.076 nM for TYK2-JH2 and 1.8 nM for JAK1-JH2, respectively. This specificity makes it suitable for research into inflammatory or autoimmune diseases [1].

JAK1/TYK2-IN-5 (compound A1) is an inhibitor of JAK1 and TYK2, exhibiting Ki values of 0.0044 nM for TYK2JH2, 0.02 nM for JAK1 JH2, 6.9 μM for JAK1 JH1, 0.79 μM for JAK2 JH1, 0.21 μM for JAK3 JH1, and 0.55 μM for TYK2JH1. Additionally, it inhibits STAT activation mediated by TYK2/JAK1, induced by IFNα.

TYK2-IN-11 (Compound 5B) is a potent and selective inhibitor of Tyk-2, with IC50 values of 0.016 nM for TYK2-JH2 and 0.31 nM for JAK1-JH2. This compound shows potential for advancing research in inflammatory and autoimmune diseases [1].