JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selectiveJAK2inhibitor with anIC₅₀of 22.86 μg/mL. JAK2-IN-6 shows no activity againstJAK1andJAK3. JAK2-IN-6 has anti-proliferative effect againstcancercells^[1].

JAK2-IN-6 (Compound B2; 6.3-50 μg/mL; 48 hours; PC-9, H1975 and PANC-1 cells) treatment exhibits significantly antiproliferative activity against all of these cancer cell lines, with IC50values of 18.1 μg/mL, 58.3 μg/mL, 40.6 μg/mL against PC-9, H1975 and PANC-1, respectively^[1].
JAK2-IN-6 (Compound B2), an intramolecular hydrogen bond is formed, holding the chlorothiophene substituent coplanar with the aminothiazole core. The chlorothiophene moiety is found to be located in the binding pocket adjacent to Val863 and Leu983, and extends towards the Asp994 of activation loop and the Gly993 of glycine-rich loop^[1].

335.83

Solid

C₁₄H₁₀ClN₃OS₂

353512-04-6

Room temperature in continental US; may vary elsewhere.