tyk2 jh1

Ropsacitinib (PF-06826647) is a selective TYK2 inhibitor, which binds to TYK2 catalytically active JH1 domain (IC50: 17 nM).

NVP-BSK805 (BSK 805) is an ATP-competitive JAK2 inhibitor.

TyK2-IN-2 is a selective inhibitor of TYK2 (IC50s: 7 nM, 0.1 μM, and 0.05 μM for TYK2 JH2, IL-23, and IFNα).

Tyk2-IN-5 is a selective and orally active inhibitor of Tyk2 JH2 (Ki: 0.086 nM for Tyk2 JH2; IC50: 25 nM for IFNα).

Tyk2-IN-7 is an inhibitor of TYK2 JH2, binds to the TYK2 JH2 domain (IC50: 0.00053 μM; Ki.app: 0.00007 μM).

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.

NVP-BSK805 trihydrochloride is a potent ATP-competitive inhibitor of JAK2, exhibiting IC50 values of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM against JAK2 JH1, JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.