PX-478 is a potent, selective inhibitor of HIF-1α and HIF-1 transcription factor activity.
PX-478 inhibits the hypoxia-induced increase in HIF-1α protein in PC-3, MCF-7, HT-29 and Panc-1 with IC50 of 3.9, 4.0, 19.4 and 10.1 nM, respectively.
PX-478 suppresses HIF-1α levels in HT-29 human colon cancer xenografts and inhibits the expression of HIF-1 target genes including VEGFR and the glucose transporter-1.
