2. Metabolic Enzyme/Protease Anti-infection
  3. HIF/HIF Prolyl-Hydroxylase Antibiotic Bacterial
  4. Echinomycin

Echinomycin  (Synonyms: Quinomycin A; NSC-13502)

Cat. No.: HY-106101 Purity: 98.57%
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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.

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

Echinomycin

Echinomycin Chemical Structure

CAS No. : 512-64-1

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Based on 11 publication(s) in Google Scholar

Echinomycin Related Antibodies

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  • Biological Activity

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  • Customer Review

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].

Cellular Effect
Cell Line Type Value Description References
B16 IC50
0.4 μg/mL
Compound: Echinomycin
Inhibitory activity against growth of B16 mouse myeloma cell line was determined by MTT assay
Inhibitory activity against growth of B16 mouse myeloma cell line was determined by MTT assay
[PMID: 14698199]
B16 IC50
6.5 x 10-8 μg/mL
Compound: 5
In vitro cytotoxicity against B16 tumor cell lines.
In vitro cytotoxicity against B16 tumor cell lines.
[PMID: 9871531]
BeWo IC50
1 μg/mL
Compound: Echinomycin
Inhibitory activity against growth of BeWO placental tumor cell line was determined by MTT assay
Inhibitory activity against growth of BeWO placental tumor cell line was determined by MTT assay
[PMID: 14698199]
CCRF-CEM IC50
0.5 μM
Compound: Echinomycin
Cytotoxicity in human leukemic CCRF-CEM cells.
Cytotoxicity in human leukemic CCRF-CEM cells.
[PMID: 14667232]
HCT-116 IC50
< 0.003 μM
Compound: 1
Cytotoxicity against human HCT116 cells
Cytotoxicity against human HCT116 cells
[PMID: 19185486]
HT-29 IC50
2.2 μg/mL
Compound: Echinomycin
Inhibitory activity against growth of HT-29 colon tumor cell line was determined by MTT assay
Inhibitory activity against growth of HT-29 colon tumor cell line was determined by MTT assay
[PMID: 14698199]
Huh-7 CC50
> 10 μM
Compound: GNF-Pf-1958
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
[PMID: 18579783]
P388 IC50
4.3 x 10-5 μg/mL
Compound: 5
In vitro cytotoxicity against P388 tumor cell lines.
In vitro cytotoxicity against P388 tumor cell lines.
[PMID: 9871531]
PANC-1 IC50
1.8 μg/mL
Compound: Echinomycin
Inhibitory activity against growth of PANC-1 tumor cell line was determined by MTT assay
Inhibitory activity against growth of PANC-1 tumor cell line was determined by MTT assay
[PMID: 14698199]
SNU-16 IC50
1.5 x 10-7 μg/mL
Compound: 5
In vitro cytotoxicity against SNU16 tumor cell lines.
In vitro cytotoxicity against SNU16 tumor cell lines.
[PMID: 9871531]
U-251 EC50
1.2 nM
Compound: 19, NSC-13502
Binding affinity to HIF-1 5'-CGTG-3' DNA sequence in human U251 cells assessed as inhibition of HRE-mediated reporter activation
Binding affinity to HIF-1 5'-CGTG-3' DNA sequence in human U251 cells assessed as inhibition of HRE-mediated reporter activation
[PMID: 22305612]
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].

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

Echinomycin Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

[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
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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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 --- --- ---
View the Complete Stock Solution Preparation Table

* 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.57%

SDS (645 KB)

COA (253 KB) HNMR (164 KB) RP-HPLC (88 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9081 mL 4.5403 mL 9.0805 mL 22.7013 mL
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Echinomycin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Echinomycin512-64-1Quinomycin A NSC-13502NSC13502NSC 13502NSC-13502HIF/HIF Prolyl-HydroxylaseAntibioticBacterialHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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