1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. Echinomycin

Echinomycin (Synonyms: Quinomycin A; NSC-13502)

Cat. No.: HY-106101
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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.

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Echinomycin Chemical Structure

Echinomycin Chemical Structure

CAS No. : 512-64-1

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Description

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].

In Vitro

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].

RT-PCR[1]

Cell Line: U251 cells
Concentration: 0 nM, 0.625 nM, 1.25 nM, 5 nM, 10 nM
Incubation Time: 16 hours
Result: Significantly inhibited VEGF mRNA expression induced by hypoxia in a dose-dependent fashion.
In Vivo

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].

Animal Model: NOD-SCID mice received 1.8Gy of irradiation and i.v. injection with peripheral blood cells from patients AML-71 and AML-150[2]
Dosage: 10 μg/kg
Administration: Intravenous injection; for 40 days
Result: Efficiently eradicated mouse lymphoma and serially transplantable human AML in xenogeneic model by preferential elimination of CSCs.
Molecular Weight

1101.26

Formula

C₅₁H₆₄N₁₂O₁₂S₂

CAS No.

512-64-1

SMILES

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

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Keywords:

EchinomycinQuinomycin ANSC-13502NSC13502NSC 13502HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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Echinomycin
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