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Echinomycin

Cat. No. 5520 1 Citation Submit a Review Datasheet / COA / SDS
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Description: Highly potent and selective HIF-1α inhibitor
Alternative 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
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for Echinomycin

Echinomycin 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.

Technical Data for Echinomycin

M. Wt 1101.26
Formula C51H64N12O12S2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 512-64-1
PubChem ID 91826096
InChI Key AUJXLBOHYWTPFV-LDUXBRJQSA-N
Smiles O=C(N[C@](C(N[C@H](C(N(C)[C@@](C(SC[C@@](N(C)C([C@H](C)NC4=O)=O)([H])C3=O)SC)([H])C(N(C)[C@@H]([C@@H](C)C)C(OC[C@]([H])4NC(C5=CN=C(C=CC=C6)C6=N5)=O)=O)=O)=O)C)=O)([H])COC([C@H]([C@@H](C)C)N3C)=O)C2=NC1=CC=CC=C1N=C2

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.

Solubility Data for Echinomycin

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 5 5

Preparing Stock Solutions for Echinomycin

The following data is based on the product molecular weight 1101.26. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.05 mM 18.16 mL 90.81 mL 181.61 mL
0.25 mM 3.63 mL 18.16 mL 36.32 mL
0.5 mM 1.82 mL 9.08 mL 18.16 mL
2.5 mM 0.36 mL 1.82 mL 3.63 mL

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Product Datasheets for Echinomycin

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for Echinomycin

References are publications that support the biological activity of the product.

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

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

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

If you know of a relevant reference for Echinomycin, please let us know.

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1 Citation for Echinomycin

Citations are publications that use Tocris products. Selected citations for Echinomycin include:

David H et al (2020) Oxygen Tension and the VHL-Hif1α Pathway Determine Onset of Neuronal Polarization and Cerebellar Germinal Zone Exit. Neuron 106 607-623.e5 PMID: 32183943

Do you know of a great paper that uses Echinomycin from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Cancer Metabolism Research Product Guide

Cancer Metabolism Research Product Guide

This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including:

Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.