PPARγ agonist17 (Compound C1) is an orally active PPARγ agonist. It enhances PPARγ activity, arrests the cell cycle of HT-29 cells at the G2/M phase, inhibits cell migration, and induces apoptosis. PPARγ agonist17 exhibits broad-spectrum antiproliferative activity against cancer cells with relatively low toxicity to normal cells and does not cross the blood-brain barrier.

PPARγ agonist 17 demonstrates strong anti-proliferative activity against HCT-116, HT-29, HCT-8, MCF-7, and MDA-MB-231 cells at concentrations of 0-1000 μM over 48 hours, while sparing 293T and L02 cells. At 4-8 μM, it significantly enhances PPARγ activity in HT-29 cells. Moreover, PPARγ agonist 17 at 2-8 μM for 24 hours effectively inhibits HT-29 cell proliferation by reducing the proportion of EdU-positive cells, causing cell cycle arrest at the G2/M phase, and downregulating cyclin D1 and CDK4 expression. It also suppresses HT-29 colony formation in both number and size in a dose-dependent manner, inducing apoptosis. In addition, PPARγ agonist 17 at 2-4 μM over 0-48 hours inhibits the migration of HT-29 cells.