jak3-in-11

JAK3-IN-11 (Compound 12) exhibits potent, noncytotoxic, irreversible, orally active JAK3 inhibitory activity (IC50 = 1.7 nM) with an excellent selectivity profile (>588-fold compared to other JAK isoforms), covalently binds to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T-cell proliferation which is a promising tool for studying autoimmune diseases [1].

JAK-IN-39 (compound 11) is a JAK inhibitor with IC50 values of 0.05 nM for JAK1, 1.18 nM for JAK2, and 0.03 nM for JAK3. It reduces cell viability in TF-1 cells and inhibits the production of TNFα and INFγ in lymphocytes in vitro.

Decernotinib (VRT-831509)(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.

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.