2. Cell Cycle/DNA Damage NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  3. Topoisomerase Reactive Oxygen Species (ROS) Apoptosis MDM-2/p53 Caspase Bcl-2 Family
  4. 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.

Topo I/II-IN-3

Topo I/II-IN-3 Chemical Structure

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Topo I/II-IN-3 Related Antibodies

Top Publications Citing Use of Products

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Topoisomerase Topo I Topo II DNA gyrase

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

View All Bcl-2 Family Isoform Specific Products:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • Biological Activity

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  • References

  • Customer Review

Description

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[1].

IC50 & Target[1]

Topoisomerase I

8.99 ()

Topoisomerase II

26.92 ()

Caspase-9

 

Caspase-3

 

Bax

 

In Vitro

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.

Topo I/II-IN-3 Related Antibodies

Western Blot Analysis[1]

Cell Line: MCF-7
Concentration: 0, 0.3, 0.6, 1.2 μM
Incubation Time: 24 h
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.

Cell Proliferation Assay[1]

Cell Line: MCF-7
Concentration: 0, 0.25, 0.5, 1 μM
Incubation Time: 48 h
Result: Significantly impaired clonogenicity in a dose-dependent manner; at 1 μM, colony formation fell to below 20% of the control.

Cell Migration Assay [1]

Cell Line: MCF-7
Concentration: 0, 0.25, 0.5, 1 μM
Incubation Time: 24 h, 48 h
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.

Cell Cycle Analysis[1]

Cell Line: MCF-7
Concentration: 0, 0.3, 0.6, 1.2 μM
Incubation Time: 24 h
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.

Apoptosis Analysis[1]

Cell Line: MCF-7
Concentration: 0, 0.3, 0.6, 1.2 μM
Incubation Time: 24 h
Result: Significantly induced apoptosis in a dose-dependent manner; at 1.2 μM, the total apoptosis rate reached approximately 40%, comparable to positive controls.
Molecular Weight

414.56

Formula

C23H35FN6
SMILES

NC(N/N=C/CCCC1C2C3C(CCCN3CCC2)CN1CC4=CC=C(F)C=C4)=N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Topo I/II-IN-3 Related Classifications

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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:

Topo I/II-IN-3TopoisomeraseReactive Oxygen Species (ROS)ApoptosisMDM-2/p53CaspaseBcl-2 Familyhuman Topo IIbreast cancerMCF-7liver cancerMDA-MB-231gastric cancertopoisomerase Itopoisomerase IIHepG2human Topo IInhibitorinhibitorinhibit

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