In cells, STA-21 inhibits Stat3 DNA binding activity, Stat3 dimerization, and Stat3-dependent luciferase activity. STA-21 remarkably inhibits the growth and the survival of the breast carcinoma cells MDA-MB-231, MDA-MB-435s, and MDA-MB-468 that express persistently activated Stat3. In RH30 and RD2 cells, STA-21 also inhibits cell viability and growth and induced apoptosis through caspases 3, 8 and 9 pathways.
In vivo
In IL-1Ra–KO mice, STA-21 (0.5 mg/kg, i.p.) reduces the arthritis score and the incidence of arthritis by decreasing the proportion of Th17 cells and increasing the proportion of Treg cells expressing FoxP3.