Ropsacitinib (PF-06826647, Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO).
PF-06826647 is a potent TYK2 inhibitor binding to the JH1 domain. PF-06826647 inhibits ear swelling in the imiquimod-induced skin inflammation model.[2]
[1] Stephen T Wrobleski, et al. J Med Chem. 2019 Oct 24;62(20):8973-8995. [2] Brian S Gerstenberger, et al. J Med Chem. 2020 Nov 25;63(22):13561-13577. [3] Gerstenberger BS, et al. J Med Chem. 2020 Nov 25;63(22):13561-13577.