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.