1. Cell Cycle/DNA Damage Apoptosis
  2. Topoisomerase Apoptosis Bcl-2 Family
  3. Topoisomerase II inhibitor 23

Topoisomerase II inhibitor 23 is a potent topoisomerase II inhibitor (IC50 = 0.94 μM). Topoisomerase II inhibitor 23 shows high selectivity and exceptional cytotoxic activity in MCF-7, HepG2, and HCT116 cells. Topoisomerase II inhibitor 23 induces cell cycle arrest at the G1 phase, leading to inhibition of cell proliferation. Topoisomerase II inhibitor 2 induces apoptosis by up-regulating the pro-apoptotic Bax level and down-regulating the anti-apoptotic Bcl-2 level[1].

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Topoisomerase II inhibitor 23 Chemical Structure

Topoisomerase II inhibitor 23 Chemical Structure

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Description

Topoisomerase II inhibitor 23 is a potent topoisomerase II inhibitor (IC50 = 0.94 μM). Topoisomerase II inhibitor 23 shows high selectivity and exceptional cytotoxic activity in MCF-7, HepG2, and HCT116 cells. Topoisomerase II inhibitor 23 induces cell cycle arrest at the G1 phase, leading to inhibition of cell proliferation. Topoisomerase II inhibitor 2 induces apoptosis by up-regulating the pro-apoptotic Bax level and down-regulating the anti-apoptotic Bcl-2 level[1].

In Vitro

Topoisomerase II inhibitor 23 (Compound, IId) shows exceptional cytotoxic activity against MCF-7 (IC50 = 24.52 μM), HepG2 (IC50 = 28.92 μM), and HCT116 cells (IC50 = 54.38 μM) [1].

Topoisomerase II inhibitor 23 shows high selectivity towards MCF-7 cells, HepG2 and HCT116 cells with SI of 3.8. 3.3 and 1.7 on the human cell line BJ cell[1].

Topoisomerase II inhibitor 23 (24.52 μM, 24 h) exhibits cell growth arrest at the G1 phase, leading to inhibition of cell proliferation in MCF-7 cells[1].

Topoisomerase II inhibitor 23 (24.52 μM, 24 h) induces apoptosis by up-regulating the pro-apoptotic Bax level and down-regulating the anti-apoptotic Bcl-2 level in MCF-7 cells[1].

Topoisomerase II inhibitor 23 shows potent topoisomerase II inhibitory activity (IC50 = 0.94 μM), higher than that of Doxorubicin (HY-15142A) (IC50 = 3.08 μM)[1].

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

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 24.52 μM
Incubation Time: 24 h
Result: Increased the percentage of cells at G0/G1 to 84.13 % in comparison to the control (61.09%).
Induced a lower reduction in the cell percentage of cells at S phase (30.56 %) than Doxorubicin (HY-15142A) (12.32 %).
Decreased population of cells at G2/M phase (3.55 %) than the control (9.27 %).

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 24.52 μM
Incubation Time: 24 h
Result: Increased annexin-V positive apoptotic cells at the early and late apoptotic stages and necrosis percentage.
Significantly up-regulated the pro-apoptotic Bax expression level by 6.96 fold and down-regulated the anti-apoptotic Bcl-2 expression level by 0.23 fold.
Molecular Weight

531.46

Formula

C28H23BrN2O2S

SMILES

CC1=CC=C(C2=CSC3=NC(C4=CC=CC=C4)=C(C(OCC)=O)C(C5=CC=C(Br)C=C5)N32)C=C1

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  • 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.

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Product Name:
Topoisomerase II inhibitor 23
Cat. No.:
HY-174404
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