DNA/TOP2A-IN-1
DNA/TOP2A-IN-1 is an inhibitor of DNA and TOP2A. DNA/TOP2A-IN-1 selectively binds to TOP2A, not TOP2B, and interacts with DNA and TOP2A to form a stable DM1-TOP2A-DNA ternary complex. DNA/TOP2A-IN-1 induces DNA damage, increases reactive oxygen species (ROS) and triggers apoptosis in triple-negative breast cancer (TNBC) cells. DNA/TOP2A-IN-1 disrupts microtubule distribution and induces cell cycle arrest. DNA/TOP2A-IN-1 shows strong antiproliferative activity and inhibits cell migration. DNA/TOP2A-IN-1 inhibits tumor growth and can be used for TNBC research.
For research use only. We do not sell to patients.
- Formula: C32H29N5O4
- Molecular Weight:547.60
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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
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- References
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Biological Activity
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topoisomerase II alpha |
DNA/TOP2A-IN-1 (Compound DM1) can directly bind to TOP2A and disrupts DNA secondary structure[1].
DNA/TOP2A-IN-1 (0-1.6 μM, 24 h) binds to DNA in 4T1 cells, facilitating the formation of a ternary DM1-TOP2A-DNA complex and induces cellular damage[1].
DM1 (10-100 μM, 37 °C for 30 min) inhibits TOP2A activity by suppressing TOP2A-mediated DNA relaxation[1].
DNA/TOP2A-IN-1 (48 h) inhibits proliferation of various cancer cells , with IC50s of 1.12 μM (4T1), 2.53 μM (MDA-MB-231), 2.68 μM (MDA-MB-468), 5.02 μM (MCF-7), 3.80 μM (Hela), 3.44 μM (SiHa), 4.78 μM (PC9), 3.68 μM (A549), 2.7 μM (ID8), 2.69 μM (PANC1) and 9.03 μM (BEAS-2B)[1].
DNA/TOP2A-IN-1 dose- dependently inhibits 4T1 and MDA-MB-231 cell viability (0-4 μM, 24-72 h), proliferation (0-3 μM, 3 days) and migration (0-12 μM, 24 h)[1].
DNA/TOP2A-IN-1 (0-2.4 μM, 24 h) exhibits collapsed and disintegrated microfilaments in 4T1 and MDA-MB-231 cells, along with altered actin and microtubule distribution[1].
DNA/TOP2A-IN-1 (0-7.2 μM, 0-48 h) promotes apoptosis and elevates intracellular reactive oxygen species in 4T1 cells and MDA-MB-231 cells[1].
DNA/TOP2A-IN-1 (0-12 μM, 24 h) induces cell cycle arrest at G2/M phase in 4T1 and MDA-MB-231 cells[1].
DNA/TOP2A-IN-1 (2 and 10 μM, 6 days ) significant inhibits breast cancer growth in organoids[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:4T1 and MDA-MB-231 cells
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Concentration:4T1: 1.2 μM, MDA-MB-231: 2.4 μM
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Incubation Time:24 h
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Result:Induced collapsed and disintegrated microfilaments in 4T1 and MDA-MB-231 cells, along with altered actin and microtubule distribution (Confocal immunofluorescence).
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Cell Line:4T1 cells
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Concentration:1.2, 1.4, 1.6 μM
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Incubation Time:24 h
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Result:Markedly increased γ-H2AX expression.
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Cell Line:4T1 cells
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Concentration:1, 1.5, 2, 2.5, 3 μM
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Incubation Time:48 h for Annexin V-FITC staining; 0, 6, 12, 18, 24, 30 h for TUNEL staining; 0, 24, 30, 36, 42 h for WB
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Result:Increased the percentage of apoptotic 4T1 cells from 15.12 % to 83.44 %.
Increased the TUNEL level over time.
Increased cleaved PARP and cleaved Caspase3, and decreased pro-Caspase9 protein level.
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Cell Line:4T1 and MDA-MB-231 cells
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Concentration:4T1: 1, 1.5, 2, 2.5, 3 μM; MDA-MB-231: 4, 6, 8, 10, 12 μM
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Incubation Time:24 h
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Result:Increased pcentage of cells in the G2/M phase and decreased the percentage of cells in the G0/G1 phase.
Downregulation of CDK4, CDK6, cyclin D, cyclin B and p-cdc2 (CDK1) protein expression level.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Balb/c mice (5 weeks old, 16-18 g) injected subcutaneously with 4T1 cells[1]
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Dosage:20 and 30 mg/kg
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Administration:i.p., every two days for 14 days
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Result:Inhibited tumor growth, with mean Tumor Growth Inhibition (TGI) of 80.76 % (30 mg/ kg) and 71.50 % (20 mg/kg).
Lowered the proportion of Ki67-positive tumor cells than in the solvent control group.
Revealed no significant drug-induced damage to the hearts, livers, spleens, lungs, and kidneys of the mice.
Chemical Information
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Molecular Weight 547.60
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Formula C32H29N5O4
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SMILES
COC1=CC=C(C=C1)OC2=C(C(C)=NN2C)CNC(C3=CC4=C(C(C5=CC=C(C=C5)OC)=N3)NC6=CC=CC=C64)=O
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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)
DNA/TOP2A-IN-1 Related Classifications
HY-175834 Related Classifications
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