1. Cell Cycle/DNA Damage
  2. Topoisomerase
  3. Topoisomerase II inhibitor 4

Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect.

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Topoisomerase II inhibitor 4 Chemical Structure

Topoisomerase II inhibitor 4 Chemical Structure

CAS No. : 2560590-49-8

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Description

Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect[1].

IC50 & Target

Topoisomerase II

 

Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
0.4 μM
Compound: E17
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
[PMID: 33191085]
HeLa IC50
0.6 μM
Compound: E17
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
[PMID: 33191085]
SW480 IC50
0.3 μM
Compound: E17
Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
[PMID: 33191085]
In Vitro

Topoisomerase II inhibitor 4 (compound E17) inhibits cancer cells with IC50 values of 4.55 μM (MDA-MB-231), 6.61 μM (A549), 2.18 μM (KG1)[1].
Topoisomerase II inhibitor 4 (1 μM; 0-22 h) induces G2/M cell cycle arrest[2].
Topoisomerase II inhibitor 4 (5 μM; 4 h) inhibits topo II-mediated chromosomes condensation in CRC cells, while also (100 μM; 0.5, 1, 2 h) induces topo II–DNA complex accumulation without degradation of topo II[2].
Topoisomerase II inhibitor 4 (1 μM; 4 h) exerts anti-tumor activity without increasing gH2AX levels in HCT116, while no DNA damage and apoptosis as well [2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Migration Assay [2]

Cell Line: HCT116, and WI-38 cells
Concentration: 0.4, 0.6, 0.8, 1.0, 1.2 μM
Incubation Time: 0, 12, 24, 48 hours
Result: Resulted migration inhibition in HCT116 and SW480 cells.

Cell Viability Assay[2]

Cell Line: HCT116, and WI-38 cells
Concentration: 0.39, 0.78, 1.56, 3.12, 6.25, 12.5, 25 μM
Incubation Time: 72 hours
Result: Exerted anti-proliferative effect in a dose-dependent manner.
Molecular Weight

459.50

Formula

C25H25N5O4

CAS No.
SMILES

O=C1C2=C(C([N+]([O-])=O)=CC=C2NC3=CC=C(CN4CCN(C)CC4)C=C3)NC5=C1C=C(O)C=C5

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    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.

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Topoisomerase II inhibitor 4
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HY-143280
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