Catalog Number: 5520
Alternate Names: Quinomycin A
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 Activity
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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 5 mM in DMSO
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. 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.
  2. Targeting HIF1α eliminates cancer stem cells in hematological malignancies.
    Wang et al.
    Cell Stem Cell, 2011;8:399
  3. Physical and functional interactions between Runx2 and HIF-1α induce vascular endothelial growth factor gene expression.
    Kwon et al.
    J.Cell.Biochem., 2011;112:3582
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