ER-400583-00 is a small-molecule HIF-1α inhibitor, inhibits the induction of HIF-1 reporter activity in response to hypoxia with IC50 of 7.9 nM.
ER-400583-00 suppressed the hypoxia-induced accumulation of the messenger RNAs (CA9, VEGFA, and SLC2A1) in U251 cells, without effect on the amount of HIF-1α protein present in U251 cells under normoxic conditions.
ER-400583-00 suppressed the induction of HIF-1α protein in response to hypoxia with IC50 of 3.7 nM.
ER-400583-00 (100 mg/kg, oral) significantly decreased mRNA levels of the HIF-1 target genes CA9, VEGFA, and SLC2A1 24 h after treatment, significantly delayed tumor growth in human U251 tumor xenografts.
ER-400583-00 suppressed cell proliferation distal to the region of blood perfusion in U251 xenograft tumors, exhibited synergistic interaction when combined with radiation therapy.
ER-400583-00 suppressed the accumulation of HIF-1α protein under hypoxic conditions but did not affect HIF-1α mRNA levels.