Echinomycin
Based on 12 publication(s) in Google Scholar
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.
- Purity : 98.57%
- CAS No.: 512-64-1
- Formula: C51H64N12O12S2
- Molecular Weight:1101.26
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Storage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications Citing Use of MedChemExpress (MCE) Echinomycin
More- Theranostics. 2025 Mar 21;15(10):4593-4613. [Abstract]
- Theranostics. 2022 Apr 4;12(7):3196-3216. [Abstract]
- Theranostics. 2022 Jan 16;12(4):1621-1638. [Abstract]
- Blood Adv. 2025 Nov 5:bloodadvances.2025016344. [Abstract]
- Sci Signal. 2023 Dec 5;16(814):eadd2282. [Abstract]
- Commun Biol. 2026 Mar 19. [Abstract]
- Cell Signal. 2026 Oct:146:112697. [Abstract]
- Oncol Rep. 2023 Dec;50(6):219. [Abstract]
- Diabetes Metab Syndr Obes. 2025 Nov 14:18:4211-4227. [Abstract]
- J Cardiovasc Dev Dis. 2025 Nov 6;12(11):438. [Abstract]
- bioRxiv. 2024 Nov 06.
- University of Sheffield. 2024 Nov 05.
All Antibiotic Isoforms
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B16 | IC50 |
0.4 μg/mL
Compound: Echinomycin
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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] |
| BeWo | IC50 |
1 μg/mL
Compound: Echinomycin
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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
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Cytotoxicity in human leukemic CCRF-CEM cells.
Cytotoxicity in human leukemic CCRF-CEM cells.
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[PMID: 14667232] |
| HCT-116 | IC50 |
<0.003 μM
Compound: 1
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Cytotoxicity against human HCT116 cells
Cytotoxicity against human HCT116 cells
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[PMID: 19185486] |
| HT-29 | IC50 |
2.2 μg/mL
Compound: Echinomycin
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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
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NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
|
[PMID: 18579783] |
| PANC-1 | IC50 |
1.8 μg/mL
Compound: Echinomycin
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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] |
| 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.
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Cell Line:U251 cells
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Concentration:0 nM, 0.625 nM, 1.25 nM, 5 nM, 10 nM
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Incubation Time:16 hours
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Result:Significantly inhibited VEGF mRNA expression induced by hypoxia in a dose-dependent fashion.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:10 μg/kg
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Administration:Intravenous injection; for 40 days
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Result:Efficiently eradicated mouse lymphoma and serially transplantable human AML in xenogeneic model by preferential elimination of CSCs.
Chemical Information
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CAS No. 512-64-1
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Appearance Solid
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Molecular Weight 1101.26
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Formula C51H64N12O12S2
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Color White to off-white
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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
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Synonyms
Quinomycin A; NSC-13502
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (12)
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Journal Impact Factor
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Most Recent
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Theranostics
FOS-driven inflammatory CAFs promote colorectal cancer liver metastasis via the SFRP1-FGFR2-HIF1 axis. [Abstract]2025 Mar 21;15(10):4593-4613. PMID: 40225580 -
Theranostics
Neuronal STAT3/HIF-1α/PTRF axis-mediated bioenergetic disturbance exacerbates cerebral ischemia-reperfusion injury via PLA2G4A. [Abstract]2022 Apr 4;12(7):3196-3216. PMID: 35547748 -
Theranostics
Piezo1-mediated mechanosensation in bone marrow macrophages promotes vascular niche regeneration after irradiation injury. [Abstract]2022 Jan 16;12(4):1621-1638. PMID: 35198061 -
Blood Adv
Hypoxia-inducible Factors Contribute to Venous Thrombosis in a Mouse Model of Myeloproliferative Neoplasms. [Abstract]2025 Nov 5:bloodadvances.2025016344. PMID: 41191539 -
Sci Signal
STAT3 palmitoylation initiates a positive feedback loop that promotes the malignancy of hepatocellular carcinoma cells in mice. [Abstract]2023 Dec 5;16(814):eadd2282. PMID: 38051779 -
Commun Biol
2026 Mar 19. PMID: 41857306 -
Cell Signal
Pan-cancer analysis reveals the prognostic relevance of NUP54 and its association with HIF-1α-related glycolytic phenotypes in lung adenocarcinoma. [Abstract]2026 Oct:146:112697. PMID: 42349706 -
Oncol Rep
P53‑microRNA interactions regulate the response of colorectal tumor cells to oxaliplatin under normoxic and hypoxic conditions. [Abstract]2023 Dec;50(6):219. PMID: 37921068 -
Diabetes Metab Syndr Obes
PEDF Alleviates Diabetic Renal Fibrosis by Degrading Kidney Ectopic Fat Deposition and Inhibiting Metabolic Reprogramming of Renal Tubular Epithelial Cells. [Abstract]2025 Nov 14:18:4211-4227. PMID: 41262465 -
J Cardiovasc Dev Dis
Role of P2X7 Receptor on Hypoxia-Induced Vascular Endothelial Growth Factor Gene Expression in H9c2 Rat Cardiomyocytes. [Abstract]2025 Nov 6;12(11):438. PMID: 41295364 -
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Solvent & Solubility
In Vitro:
DMSO : 5 mg/mL (4.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 0.5 mg/mL (0.45 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 0.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (645 KB)
- English - EN (645 KB)
- Français - FR (645 KB)
- Deutsch - DE (645 KB)
- Norwegian - NO (645 KB)
- Español - ES (645 KB)
- Swedish - SV (645 KB)
- Italian - IT (645 KB)
- Korean - KR (645 KB)
- Portuguese - PT (645 KB)
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Handling Instructions (2659 KB)
References
[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]
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 |