jak1-in-18

JAK1-IN-18 (Example 2) is a selective JAK1 inhibitor with an IC50 value of 0.15 nM, demonstrating significantly greater inhibitory potency for JAK1 compared to JAK2 and JAK3. It significantly reduces inflammation in ulcerative colitis (UC) mouse models induced by DSS and Crohn's disease (CD) rat models induced by DNBS. JAK1-IN-18 is applicable for research into autoimmune diseases (such as inflammatory bowel disease), viral infections (such as hepatitis B virus infection), and cancers (such as hematologic malignancies).

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-IN-30 (compound 31) is a water-soluble Janus kinase (JAK) inhibitor with IC50 values of 2 nM for JAK2, 15 nM for JAK1, 18 nM for JAK3, and 2 nM for TYK2, identified for its research potential in treating dry eye disease (DED) [1].