jak-in-11

JAK-IN-11 (R-348) is a potent and selective inhibitor of JAK, has the potential for the skin disorders treatment.

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].

Momelotinib (LM-1149) is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells.

JAK/HDAC-IN-4 (compound 11 i) is a dual inhibitor targeting both JAK2 and HDAC6, with IC50 values of 0.49 nM and 12 nM respectively. It inhibits cell proliferation and the production of nitric oxide. In a mouse model induced by Imiquimod, JAK/HDAC-IN-4 ameliorates psoriasiform skin lesions with low toxicity.

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.

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.