Hypoxia-inducible factor-1 (HIF-1) is a heterodimeric transcription factor composed of a HIF-1α subunit and HIF-1β subunit. The HIF-1α subunit is regulated by cellular oxygen levels and therefore plays an important role in maintaining cellular oxygen homeostasis. KC7F2 is an inhibitor of HIF-1α protein translation, but not transcription, that suppresses phosphorylation of two key regulators of protein synthesis, eukaryotic translation initiation factor 4E binding protein 1 (4EBP1) and p70 S6 kinase (S6K). It inhibits hypoxia-induced expression of several HIF target genes, such as carbonic anhydrase IX, matrix metalloproteinase 2, enolase 1, and endothelin 1. KC7F2 is cytotoxic to a variety of cancer cell lines with an IC50 value of 15-25 μM.
