IDF-11774 is a hypoxia-inducible factor-1 (HIF-1) inhibitor. It reduces the HRE-luciferase activity of HIF-1α (IC50 = 3.65 μM) and blocks HIF-1α accumulation under hypoxia in HCT116 human colon cancer cells.
IDF-11774 inhibits the accumulation of HIF-1α in vitro and in vivo in colorectal carcinoma HCT116 cells under hypoxic conditions. The treatment of IDF-11774 suppresses angiogenesis of cancer cells by reducing the expression of HIF-1 target genes, reduces glucose uptake, thereby sensitizing cells to growth under low glucose conditions, and decreases the extracellular acidification rate (ECAR) and oxygen consumption rate of cancer cells. Therefore, IDF-11774 reduces cancer cell growth through the regulation of cancer glycolytic metabolism and energy production[1].
IDF-11774 exhibited substantial anticancer efficacy in mouse models containing KRAS, PTEN, or VHL mutations, which often occur in malignant cancers[1].
[1] Ban HS, et al. Cell Death Dis. 2017, 8(6):e2843.