Topoisomerase I/II inhibitor 3

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Topoisomerase I/II inhibitor 3 (compound 7) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis by inhibiting PI3K/Akt/mTOR signaling pathway. Topoisomerase I/II inhibitor 3 can be used for liver cancer research.

For research use only. We do not sell to patients.

Topoisomerase I/II inhibitor 3 Chemical Structure

CAS No. : 2770804-74-3

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Topoisomerase Topo I Topo II

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Topoisomerase I

Topoisomerase II

PI3K

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	22.91 μM Compound: 7	Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
BGC-823	IC₅₀	18.55 μM Compound: 7	Antiproliferative activity against human BGC-823 cells measured after 72 hrs by MTT assay Antiproliferative activity against human BGC-823 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
C6	IC₅₀	12.88 μM Compound: 7	Antiproliferative activity against human C6 cells measured after 72 hrs by MTT assay Antiproliferative activity against human C6 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
HCCLM9	IC₅₀	2.1 μM Compound: 7	Antiproliferative activity against human HCCLM9 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HCCLM9 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
HCT-116	IC₅₀	11.39 μM Compound: 7	Antiproliferative activity against human HCT-116 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
HepG2	IC₅₀	25.84 μM Compound: 7	Antiproliferative activity against human HepG2 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
HGC-27	IC₅₀	12.37 μM Compound: 7	Antiproliferative activity against human HGC-27 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HGC-27 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
HT-29	IC₅₀	5.35 μM Compound: 7	Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
Huh-7	IC₅₀	1.93 μM Compound: 7	Antiproliferative activity against human Huh-7 cells measured after 72 hrs by MTT assay Antiproliferative activity against human Huh-7 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
L02	IC₅₀	68.03 μM Compound: 7	Cytotoxicity against human L02 cells measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
MGC-803	IC₅₀	19.9 μM Compound: 7	Antiproliferative activity against human MGC-803 cells measured after 72 hrs by MTT assay Antiproliferative activity against human MGC-803 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
RKO	IC₅₀	17.74 μM Compound: 7	Antiproliferative activity against human RKO cells measured after 72 hrs by MTT assay Antiproliferative activity against human RKO cells measured after 72 hrs by MTT assay	[PMID: 35462164]
SGC-7901	IC₅₀	34.79 μM Compound: 7	Antiproliferative activity against human SGC-7901 cells measured after 72 hrs by MTT assay Antiproliferative activity against human SGC-7901 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
SW480	IC₅₀	8.36 μM Compound: 7	Antiproliferative activity against human SW480 cells measured after 72 hrs by MTT assay Antiproliferative activity against human SW480 cells measured after 72 hrs by MTT assay	[PMID: 35462164]
U-87MG ATCC	IC₅₀	54.62 μM Compound: 7	Antiproliferative activity against human U87 cells measured after 72 hrs by MTT assay Antiproliferative activity against human U87 cells measured after 72 hrs by MTT assay	[PMID: 35462164]

In Vitro

Topoisomerase I/II inhibitor 3 (compound 7) (0-100 μM) can insert into DNA and change the topology of DNA, cause DNA damage to a certain extent^[1].
Topoisomerase I/II inhibitor 3 (0-4 μM, 24 h) inhibits HCC (hepatocellular carcinoma) cells proliferation in a dose-dependent manner, inhibits migration and invasion of LM9 and HuH7 cells by inhibiting the expression of MMP-9^[1].
Topoisomerase I/II inhibitor 3 (0-14 μM, 48 h) significantly induces the apoptosis of LM9 and HuH7 cells, and induces mitochondrial dysfunction and ROS burst in a dose-dependent manner^[1].
Topoisomerase I/II inhibitor 3 (0-7 μM, 48 h) reduces the expression of the inhibitory factor Bcl-2 and promotes the expression of mitochondria-dependent apoptosis-related proteins such as Bax, cytochrome C, cleaved-caspase-3 and cleaved-caspase-9; inhibits the phosphorylation of PI3K/Akt/mTOR signaling pathway^[1].

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

Cell Proliferation Assay

Cell Line:	HCC cells (HuH7 and LM9)^[1]
Concentration:	0, 0.5, 1, 2, and 4 μM
Incubation Time:	24 h
Result:	Inhibited HCC cells proliferation in a dose-dependent manner, with IC₅₀ values of 2.10 μM (LM9) and 1.93 μM (HuH7), respectively, and dose-dependently inhibited the formation of cell colonies.

Apoptosis Analysis

Cell Line:	LM9 and HuH7 cells^[1]
Concentration:	0, 1.8, 3.5, 7, and 14 μM
Incubation Time:	48 h
Result:	Significantly induced the apoptosis of LM9 and HuH7 cells in a concentration-dependent manner.

Western Blot Analysis

Cell Line:	LM9 and HuH7 cells^[1]
Concentration:	0, 1.8, 3.5, and 7 μM
Incubation Time:	48 h
Result:	Reduced the expression of the inhibitory factor Bcl-2 and promoted the expression of mitochondria-dependent apoptosis-related proteins such as Bax, cytochrome C, cleaved-caspase-3 and cleaved-caspase-9; inhibited the phosphorylation of PI3K/Akt/mTOR signaling pathway.

In Vivo

Topoisomerase I/II inhibitor 3 (compound 7) (male Kunming mice, 0-400 mg/kg, IP, once) causes the mice in the 400 mg/kg group die, with the LD₅₀ between 250 and 400 mg/kg^[1].

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

Animal Model:	Male Kunming mice (19-22 mg, 8 mice, 4 groups)^[1]
Dosage:	200, 250, 400 mg/kg (dissolved in 5% DMSO and castor oil)
Administration:	IP, once
Result:	Did not cause the mice in the 250 mg/kg and 200 mg/kg groups die after 2 weeks of administration, and caused the mice in the 400 mg/kg group die, with the LD₅₀ between 250 and 400 mg/kg.

Molecular Weight

404.46

Formula

C₂₄H₂₄N₂O₄

CAS No.

2770804-74-3

SMILES

C1(C=CC2=C3C=NC(C4=CC5=C(OCO5)C=C4CN6CCCCCC6)=C2)=C3OCO1

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

Handling Instructions (2659 KB)

References

[1]. Deng X, Luo T, Zhang X, et al. Design, synthesis and biological evaluation of 3-arylisoquinoline derivatives as topoisomerase I and II dual inhibitors for the therapy of liver cancer. Eur J Med Chem. 2022;237:114376. [Content Brief]