Pomiferin, a flavonoid from the fruits of Maclura pomifera, acts as an potential inhibitor of HDAC, with an IC50 of 1.05 μM, and also potently inhibits mTOR (IC50, 6.2 µM). Pomiferin is an potential inhibitor of HDAC, with an IC50 of 1.05 μM. Pomiferin shows cytotoxic effects on human tumor cell lines, with GI50s of 1.32 ± 0.02 μM (HCT-15 cells), 2.92 ± 0.09 μM (MDA-MB-231 cells), 3.18 ± 0.05 μM (ACHN cells), 3.34 ± 0.11 μM (LOX-IMVI cells), 3.95 ± 0.05 μM (PC-3 cells), 5.14 ± 0.06 μM (NCI-H23 cells), and 123 μM (Hepatocyte cells). Pomiferin is a highly specific mTOR inhibitor, with an IC50 of 6.2 µM. Pomiferin triacetate only affects two PI3Kα mutants, E542K and E545K. Pomiferin triacetate (0.3125-20 µM) stabilizes Pdcd4 from TPA-induced degradation in HEK293 cells. Pomiferin triacetate (20 µM) inhibits IGF-1-induced signaling downstream of Akt activation. Pomiferin (5, 10 and 20 mg/kg, p.o.) shows protective effects on the treatment of reperfusion injury. Pomiferin also increases SOD activities and total antioxidative capacity, and decreases malondialdehyde in rats.