Echinomycin  (Synonyms: Quinomycin A; NSC-13502)

Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC₅₀ of 29.4 pM^[1][2].

Echinomycin (0-10 nM; 16 hours; U251 cells) treatment significantly inhibits hypoxia-induced VEGF mRNA expression in a dose-dependent fashion. Echinomycin very potently inhibits hypoxic induction of luciferase expression in U251-HRE in a dose-dependent fashion with an EC₅₀ of 1.2 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Echinomycin (10 μg/kg; intravenous injection; for 40 days; NOD-SCID mice) treatment efficiently eradicates mouse lymphoma and serially transplantable human acute myeloid leukemia (AML) in xenogeneic model by preferential elimination of cancer stem cells (CSCs). HIF1α maintains mouse lymphoma CSCs by repressing a negative feedback loop in the Notch pathway^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1101.26

C₅₁H₆₄N₁₂O₁₂S₂

512-64-1

Solid

White to off-white

[H]C1=NC2=C(N=C1C(N[C@H](COC([C@H](C(C)C)N(C)C([C@H]3N4C)=O)=O)C(N[C@@H](C)C(N(C)[C@@H]([C@@H](SC)SC3)C(N(C)[C@@H](C(C)C)C(OC[C@@H](NC(C5=NC6=C(C=CC=C6)N=C5[H])=O)C(N[C@@H](C)C4=O)=O)=O)=O)=O)=O)=O)C=CC=C2

Room temperature in continental US; may vary elsewhere.

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Kong D, et al. Echinomycin, a small-molecule inhibitor of hypoxia-inducible factor-1 DNA-binding activity. Cancer Res. 2005 Oct 1;65(19):9047-55.  [Content Brief]

  [2]. Wang Y, et al. Targeting HIF1α eliminates cancer stem cells in hematological malignancies. Cell Stem Cell. 2011 Apr 8;8(4):399-411.  [Content Brief]