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 ActivityHighly 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
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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