FG-2216 (YM-311, IOX3) is a potent, selective small molecule inhibitor of HIF prolyl hydroxylase (HIF-PHD) with IC50 of 3.9 nM (PHD2).
FG-2216 decreases protein expression of DNA/RNA demethylase FTO (in C2C12 cells) and reduces maximal respiration rate in vitro.
FG-2216 up-regulates HIF-1α and increases erythropoietin expression in mice, also significantly reduces bone mineral density and content and alter adipose tissue distribution in mice.
FG-2216 is orally bioavailable and induced significant and reversible Epo induction in vivo.
