Topo I/II-IN-3
Topo I/II-IN-3 is a dual inhibitor of topoisomerase I/II (topoisomerase I/II), with an IC50 of 8.99 μM against Topo I and an IC50 of 26.92 μM against Topo II. Topo I/II-IN-3 induces DNA damage, elevates intracellular ROS levels, activates the mitochondrial apoptosis pathway, and exerts cytotoxicity against cancer cells. Topo I/II-IN-3 upregulates the expression of γ-H2AX, p53, activated caspase-9, Bax and activated caspase-3, while downregulating the expression of Bcl-2. Topo I/II-IN-3 can be used in research related to breast cancer, liver cancer and gastric cancer.
For research use only. We do not sell to patients.
- Formula: C23H35FN6
- Molecular Weight:414.56
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Topoisomerase I 8.99 () |
Topoisomerase II 26.92 () |
Caspase-9 |
Caspase-3 |
Bax |
Topo I/II-IN-3 (Compound A6) (0.6-22.1 μM; 48 h) potently inhibits the proliferation of MCF-7, MDA-MB-231, HepG2 and SGC-7901 cancer cells, with IC50 values of 0.6, 12.6, 3.4 and 5.4 μM, respectively, and exhibits low cytotoxicity against normal HEK-293 cells (IC50 = 22.1 μM)[1].
Topo I/II-IN-3 (1.56-100 μM; 30 min) blocks DNA relaxation and kDNA decatenation, with IC50 values of 8.99 μM and 26.92 μM, respectively[1].
Topo I/II-IN-3 (0.3-1.2 μM; 24 h) induces dose-dependent DNA damage in MCF-7 cells, upregulates the expression of γ-H2AX, and increases the levels of p53, activated caspase-9, Bax and activated caspase-3, while downregulating Bcl-2[1].
Topo I/II-IN-3 (0.25-1 μM; 24-48 h) potently inhibits the long-term proliferation and migration of MCF-7 cells[1].
Topo I/II-IN-3 (0.3-1.2 μM; 24 h) induces dose-dependent G2/M phase arrest, triggers apoptosis, elevates intracellular ROS levels, and reduces mitochondrial membrane potential in MCF-7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7
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Concentration:0, 0.3, 0.6, 1.2 μM
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Incubation Time:24 h
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Result:Markedly upregulated γ-H2AX protein expression in a dose-dependent manner, confirming induction of DNA double-strand breaks.\nDose-dependently upregulated expression of p53, cleaved caspase-9, Bax, and cleaved caspase-3, while downregulating Bcl-2 expression.
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Cell Line:MCF-7
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Concentration:0, 0.25, 0.5, 1 μM
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Incubation Time:48 h
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Result:Significantly impaired clonogenicity in a dose-dependent manner; at 1 μM, colony formation fell to below 20% of the control.
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Cell Line:MCF-7
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Concentration:0, 0.25, 0.5, 1 μM
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Incubation Time:24 h, 48 h
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Result:Significantly reduced cell migration in a dose-dependent manner; at 1 μM, anti-migratory effects were comparable to positive controls CPT and VP-16.
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Cell Line:MCF-7
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Concentration:0, 0.3, 0.6, 1.2 μM
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Incubation Time:24 h
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Result:Induced dose-dependent G2/M phase arrest, with increasing proportions of cells in G2/M phase and decreasing proportions in G0/G1 phase as concentrations rose.
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Cell Line:MCF-7
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Concentration:0, 0.3, 0.6, 1.2 μM
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Incubation Time:24 h
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Result:Significantly induced apoptosis in a dose-dependent manner; at 1.2 μM, the total apoptosis rate reached approximately 40%, comparable to positive controls.
Chemical Information
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Molecular Weight 414.56
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Formula C23H35FN6
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SMILES
NC(N/N=C/CCCC1C2C3C(CCCN3CCC2)CN1CC4=CC=C(F)C=C4)=N
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Topo I/II-IN-3 Related Classifications
HY-183330 Related Classifications
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