Chemical Name: N-(2-Quinoxalinylcarbonyl)-O-[N-(2-quinoxalinylcarbonyl)-D-seryl-L-alanyl-3-mercapto-N,S-dimethylcysteinyl-N-methyl-L-valyl]-D-seryl-L-alanyl-N-methylcysteinyl-N-methyl-L-valine-(81)-lactone-cyclic (37)-thioether
Biological ActivityEchinomycin is a highly potent and selective HIF-1α inhibitor (IC50 = 29.4 pM). Selectively inhibits HIF-1 binding to the VEGF promoter without affecting the binding of AP-1 or NF-κB. Inhibits colony formation of cancer stem cells (CSC) with a 100-fold selectivity over normal hematopoietic progenitor cells. Eradicates mouse lymphomas and human AML xenografts by eliminating CSCs.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Echinomycin, a small-molecule inhibitor of hypoxia-inducible factor-1 DNA-binding activity.
Kong D, Park EJ, Stephen AG et al.
Cancer Res. 65(19):9047-55.
Targeting HIF1α eliminates cancer stem cells in hematological malignancies.
Wang et al.
Cell Stem Cell, 2011;8:399
Physical and functional interactions between Runx2 and HIF-1α induce vascular endothelial growth factor gene expression.
Kwon et al.
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