Cat. No. 5520

Echinomycin C51H64N12O12S2 [512-64-1]

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Alternative Name: 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

Soluble to 5 mM in DMSO
>98 %
Store at -20°C

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.

Certificate of Analysis / Safety Data Sheet

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Kwon et al (2011) Physical and functional interactions between Runx2 and HIF-1α induce vascular endothelial growth factor gene expression. J.Cell.Biochem. 112 3582. PMID: 21793044.

Wang et al (2011) Targeting HIF1α eliminates cancer stem cells in hematological malignancies. Cell Stem Cell 8 399. PMID: 21474104.

Kong et al (2005) Echinomycin, a small-molecule inhibitor of hypoxia-inducible factor-1 DNA-binding activity. Cancer Res. 65 9047. PMID: 16204079.

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Keywords: Echinomycin, supplier, Highly, potent, selective, HIF-1α, inhibitors, inhibits, cancer, stem, cells, VEGF, lymphomas, Tocris Bioscience, Hypoxia Inducible Factor Inhibitor products

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