Tyk2-IN-29

Tyk2-IN-29 (compound 2) (preincubated for 20 min followed by IL-22 stimulation for 15 min) potently inhibits STAT3 phosphorylation in IL-22 (HY-P78857)-stimulated serum-starved HT29 colon cancer cells (IC₅₀ = 16 nM, with 95.9% inhibition at 10 μM)^[1].

Tyk2-IN-29 (after 30 min preincubation followed by stimulation with IL-23 and IL-1β for 48 h) potently inhibits the production of the proinflammatory cytokine IL-17F in primary human peripheral blood-derived Th17 cells stimulated with IL-23 (HY-P74816) and IL-1β (HY-P78459) (mean IC₅₀ = 105 nM)^[1].
Tyk2-IN-29 (120 min) potently and highly selectively inhibits TYK2 kinase activity in an in vitro kinase biochemical assay system (IC₅₀ = 1.9 nM)^[1].
Tyk2-IN-29 (after 30 min pre-incubation followed by 15 min IL-23 stimulation) potently inhibits STAT3 phosphorylation in IL-23-stimulated primary human peripheral blood-derived Th17 cells (mean IC₅₀ = 51 nM)^[1].
Tyk2-IN-29 (up to 30 μM; over 7 min) exhibits minimal hERG potassium channel inhibition in stably transfected hERG-HEK cell lines (IC₅₀ > 30 μM)^[1].
Tyk2-IN-29 (compound 1) potently and highly selectively inhibits TYK2 kinase activity in in vitro kinase biochemical assays (IC₅₀ = 1.9 nM), and also inhibits JAK1/2/3 kinase activity with IC₅₀ values of 20 nM, 50 nM, and 212 nM, respectively^[2].