Isoangustone A, a natural product isolated and purified from the roots of Licorice with antitumor activity, induces G1 cycle arrest in DU145 human prostate and 4T1 murine mammary cancer cells, dampens mesangial sclerosis associated with inflammation in response to high glucose through hindering TGF-β and NF-κB signaling, inhibits cell proliferation by targeting PI3K, MKK4, and MKK7 in human melanoma and shows strong ferric reducing activities and effectively scavenged DPPH, ABTS(+), and singlet oxygen radicals.