Netropsin
Based on 1 publication(s) in Google Scholar
Netropsin is a DNA minor groove binder (MGB) and antibiotic (antibiotic). Netropsin exhibits antibacterial, antiparasitic, antiviral, and antitumor activities. Netropsin binds with high affinity to the minor groove of A-T-rich DNA sequences, competitively blocking the binding of specific transcription factors (such as HMGA1) to target gene promoters or enhancers, thereby inhibiting chromatin loop formation and downstream gene transcription. Netropsin is a Topoisomerase inhibitor that inhibits the catalytic activity of DNA Top I and II and impedes the stabilization of their DNA-protein cross-linking complexes. Netropsin can be used in research on infections, cancer, and septicemia.
For research use only. We do not sell to patients.
- CAS No.: 1438-30-8
- Formula: C18H26N10O3
- Molecular Weight:430.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Netropsin
MoreAll Antibiotic Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
Top1 |
Topoisomerase II |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| DC3F | IC50 |
3.2 mM
Compound: Netropsin
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Cytotoxicity against hamster DC-3F cells
Cytotoxicity against hamster DC-3F cells
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[PMID: 20471276] |
| HT-29 | IC50 |
44.7 μM
Compound: Netropsin
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Inhibitory concentration that reduced the viability of HT 29 cell population by 50%.
Inhibitory concentration that reduced the viability of HT 29 cell population by 50%.
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[PMID: 9003520] |
| K562 | IC50 |
>50 μM
Compound: Netropsin
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Cytotoxicity against human K562 cells after 72 hrs by MTS assay
Cytotoxicity against human K562 cells after 72 hrs by MTS assay
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[PMID: 20471276] |
| KB | IC50 |
47.1 μM
Compound: Netropsin
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Inhibitory concentration that reduced the viability of KB cell population by 50%.
Inhibitory concentration that reduced the viability of KB cell population by 50%.
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[PMID: 9003520] |
| SK-VLB | IC50 |
>10 μM
Compound: Netropsin
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Inhibitory concentration that reduced the viability of SKVLB cell population by 50%.
Inhibitory concentration that reduced the viability of SKVLB cell population by 50%.
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[PMID: 9003520] |
In Vitro
Netropsin (10-100 μM; 15 min) inhibits topoisomerase II isolated from L1210 leukemia cells in the kDNA decatenation assay, with an IC90 of 200 µM[6].
Netropsin (2 days) significantly inhibits cell migration and invasion in HCT116 colorectal cancer cells[9].
Netropsin (65-70 µM) inhibits VM-26 (HY-13761)-induced topoisomerase II cleavable complexes in mouse fibrosarcoma 935.1 cell nuclei, with an IC50 of 65 µM[6].
Netropsin hydrochloride (3-1000 μg/mL) inhibits various bacteria and C. albicans on nutrient agar plates, with MIC values ranging from 3 μg/mL against S. albus to 1000 μg/mL against Ps. aeruginosa[3].
Netropsin (10-25 μM; 24 h) dose-dependently attenuates LPS (HY-D1056)-induced NOS2 promoter activity in RAW264.7 mouse macrophages, reducing activity to 44.9% at 25 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Netropsin (25 mg/kg; i.p.; single administration, 30 min before LPS injection; observation for 90 h) improves the survival rate of wild-type mice during LPS-induced endotoxemia[2].
Netropsin (25 mg/kg; i.p.; single administration 30 min before LPS injection; observation for 90 h) does not significantly improve the survival rate of 1400W (HY-18730)-treated mice during LPS-induced endotoxemia[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (wild-type, male, 6-8 weeks of age)[2]
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Dosage:25 mg/kg
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Administration:i.p.; single dose 30 min before LPS injection; observation for 90 h
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Result:WT mice injected with LPS plus netropsin exhibited a significantly higher survival rate (36% survival) at 70-90 h following injection.
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Animal Model:C57BL/6 (wild-type, male, 6-8 weeks of age)[2]
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Dosage:25 mg/kg
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Administration:i.p.; single dose 30 min before LPS injection; observation for 90 h
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Result:1400W-treated mice receiving LPS plus netropsin did not exhibit a significant improvement in survival rates compared with those treated with LPS vehicle.
Chemical Information
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CAS No. 1438-30-8
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Molecular Weight 430.46
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Formula C18H26N10O3
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SMILES
O=C(C1=CC(NC(CNC(N)=N)=O)=CN1C)NC2=CN(C)C(C(NCCC(N)=N)=O)=C2
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Structure Classification
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Initial Source
Streptomyces netropsis
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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PLoS Pathog
Anti-orthopoxvirus drugs inhibit lumpy skin disease virus replication by targeting viral DNA polymerase. [Abstract]2026 Jan 26;22(1):e1013903. PMID: 41587213
Purity & Documentation
References
[2]. Grant MA, et al. Netropsin improves survival from endotoxaemia by disrupting HMGA1 binding to the NOS2 promoter. The Biochemical journal. 2009 Feb 15;418(1):103-12. [Content Brief]
[6]. Beerman TA, et al. Netropsin and bis-netropsin analogs as inhibitors of the catalytic activity of mammalian DNA topoisomerase II and topoisomerase cleavable complexes. Biochimica et biophysica acta. 1991 Aug 27;1090(1):52-60. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Netropsin Related Classifications
HY-N6800 Related Classifications
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