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

Topoisomerase II inhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a Type II DNA topoisomerase (topo II) inhibitor , as a topo IIα/β inhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential.

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Topoisomerase II inhibitor 3 Chemical Structure

Topoisomerase II inhibitor 3 Chemical Structure

CAS No. : 99140-25-7

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Description

Topoisomerase II inhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a Type II DNA topoisomerase (topo II) inhibitor , as a topo IIα/β inhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential[1].

IC50 & Target

IC50: 0.17 μM (topo IIα); IC50: 0.23 μM (topo IIβ)[1]

In Vitro

Topoisomerase II inhibitor 3 (Compound 6 h ) has function as a strong topo IIα/β inhibitor, causeS obvious DNA damage, and induces apoptosis by triggering the loss of mitochondrial membrane potential.
Topoisomerase II inhibitor 3 (Compound 6 h ) is a topo IIα/β dual inhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypesl.
Topoisomerase II inhibitor 3 (Compound 6 h ) also can induce the formation of DSBs in a does-dependent manner[1].

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

Cell Proliferation Assay[1]

Cell Line: Human breast cancer MDA-MB-231 cells; human lung cancer A549; human acute myelogenous leukemia KG1 cells; rat myocardial H9C2 cells
Concentration: 100 μM
Incubation Time: 12 h
Result: Exerted the most potent anti-proliferative activity in MDA-MB-231 cells (IC50: 0.42 μM), A549 cells (IC50: 1.10 μM), KG1 cells (IC50: 0.15 μM) and H9C2 cells (IC50 >20 μM).

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5-10 μM
Incubation Time: 24 h
Result: Caused obvious loss of mitochondrial membrane potential (MMP) in MDA-MB-231 cells.
Molecular Weight

356.38

Formula

C18H20N4O4

CAS No.
SMILES

O=C1C2=C(C([N+]([O-])=O)=CC=C2NCCCN(C)C)NC3=C1C=C(O)C=C3

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Topoisomerase II inhibitor 3
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HY-143279
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