EED-IN-3 is an orally active inhibitor of EED. It effectively binds with EED (IC50 = 0.62 μM) to inhibit PRC2 and reduces H3K27me3 levels. EED-IN-3 selectively inhibits PC3 cells with an IC50 of 3.69 μM and significantly suppresses colony formation and migration. This compound is useful for prostate cancer research.

EED-IN-3 (Compound 39) (7 days) exhibits highly selective anticancer activity against PC3 cells and demonstrates low toxicity to normal cells. EED-IN-3 (0-16 μM) significantly reduces H3K27me3 levels in PC3 cells. At concentrations of 0-16 μM for 24 or 48 hours, EED-IN-3 inhibits the migration and invasion of PC3 cells in a time- and concentration-dependent manner. Moreover, EED-IN-3 (8-16 μM, 12 days) substantially suppresses colony formation in PC3 cells.

EED-IN-3 (Compound 39) (single dose 2 g/kg; i.g.) shows relatively low toxicity in C57BL/6 wild-type mice. EED-IN-3 administered at 50 mg/kg to 100 mg/kg via i.g., once daily for 14 days, significantly inhibits the growth of tumors in BALB/C-nu mice injected with PC3 cells.