tyk2 in 5

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).

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-20 (Example 289) is an effective inhibitor of Tyk2 with an IC50 value below 5 nM. Additionally, it inhibits JAK1, JAK2, and JAK3 with IC50 values under 100 nM. This compound is utilized for the research of inflammatory diseases.

DEL1187-126-5-80 is a JAK3 inhibitor, exhibiting IC50 values of 52 nM and 7.9 nM for JAK3WT at 0 and 60 minutes, respectively. It shows no activity against the C909S mutant, JAK1, JAK2, and TYK2, and can be utilized in research on immune-mediated diseases.

Gusacitinib-d4 (ASN-002-d4) is the deuterium-labeled form of Gusacitinib. Gusacitinib (ASN-002) is an orally effective dual kinase inhibitor targeting SYK and JAK. It exhibits IC50 values of 5, 46, 4, 11, and 8 nM for SYK, JAK1, JAK2, JAK3, and TYK2, respectively. This compound effectively and rapidly suppresses key inflammatory pathways involved in the pathogenesis of atopic dermatitis. Gusacitinib is also used in research for conditions such as chronic hand eczema and basal cell carcinoma.