JAK2-IN-6, a polysubstituted aminothiazole derivative, is a potent and selective inhibitor of JAK2 (ic50 at 22.86 μg/mL). Jak2-in-6 inhibits the activity of JAK2 enzymes by interfering with Jak2-related signaling pathways, thereby producing therapeutic effects on the specific disease IN which JAK2 is dysregulated, and does not show activity on JAK1 and JAK3. JAK2 is a protein involved in signaling pathways that regulate cell growth and division. Abnormal activation of JAK2 has been linked to a variety of diseases, including some types of cancer and inflammatory diseases. JAK2-IN-6 has antiproliferative activity against cancer cells.

JAK2:22.86 μg/mL

The treatment of JAK2-IN-6 (Compound B2; 6.3-50 μg/mL; 48 hours) demonstrates significant antiproliferative activity against PC-9, H1975, and PANC-1 cell lines. The IC50 values for PC-9, H1975, and PANC-1 cell lines are 18.1 μg/mL, 58.3 μg/mL, and 40.6 μg/mL, respectively [1].