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

Echinomycin (Synonyms: Quinomycin A; NSC-13502)

Cat. No.: HY-106101 Purity: ≥98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

Echinomycin Chemical Structure

Echinomycin Chemical Structure

CAS No. : 512-64-1

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Estimated Time of Arrival: December 31
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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].

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

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].

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

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 5.3 mg/mL (4.81 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9081 mL 4.5403 mL 9.0805 mL
5 mM --- --- ---
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: ≥98.0%

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Keywords:

EchinomycinQuinomycin A NSC-13502NSC13502NSC 13502NSC-13502HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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Product Name:
Echinomycin
Cat. No.:
HY-106101
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