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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1438-30-8
- 分子式: C18H26N10O3
- 分子量:430.46
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
MedChemExpress(MCE)の使用を引用している文献 Netropsin
MoreAntibiotic アイソフォーム固有の製品をすべて表示
MoreDNA/RNA Synthesis アイソフォーム固有の製品をすべて表示
MoreParasite アイソフォーム固有の製品をすべて表示
MoreTopoisomerase アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
[1]|
Top1 |
Topoisomerase II |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| DC3F | IC50 |
3.2 mM
Compound: Netropsin
|
Cytotoxicity against hamster DC-3F cells
Cytotoxicity against hamster DC-3F cells
|
[PMID: 20471276] |
| HT-29 | IC50 |
44.7 μM
Compound: Netropsin
|
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%.
|
[PMID: 9003520] |
| K562 | IC50 |
>50 μM
Compound: Netropsin
|
Cytotoxicity against human K562 cells after 72 hrs by MTS assay
Cytotoxicity against human K562 cells after 72 hrs by MTS assay
|
[PMID: 20471276] |
| KB | IC50 |
47.1 μM
Compound: Netropsin
|
Inhibitory concentration that reduced the viability of KB cell population by 50%.
Inhibitory concentration that reduced the viability of KB cell population by 50%.
|
[PMID: 9003520] |
| SK-VLB | IC50 |
>10 μM
Compound: Netropsin
|
Inhibitory concentration that reduced the viability of SKVLB cell population by 50%.
Inhibitory concentration that reduced the viability of SKVLB cell population by 50%.
|
[PMID: 9003520] |
体外実験
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6 (wild-type, male, 6-8 weeks of age)[2]
-
Dosage:25 mg/kg
-
Administration:i.p.; single dose 30 min before LPS injection; observation for 90 h
-
Result:WT mice injected with LPS plus netropsin exhibited a significantly higher survival rate (36% survival) at 70-90 h following injection.
-
Animal Model:C57BL/6 (wild-type, male, 6-8 weeks of age)[2]
-
Dosage:25 mg/kg
-
Administration:i.p.; single dose 30 min before LPS injection; observation for 90 h
-
Result:1400W-treated mice receiving LPS plus netropsin did not exhibit a significant improvement in survival rates compared with those treated with LPS vehicle.
化学情報
-
CAS 番号 1438-30-8
-
分子量 430.46
-
分子式 C18H26N10O3
-
SMILES
O=C(C1=CC(NC(CNC(N)=N)=O)=CN1C)NC2=CN(C)C(C(NCCC(N)=N)=O)=C2
-
Structure Classification
-
Initial Source
Streptomyces netropsis
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
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
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)