Topoisomerase I/II inhibitor 2

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Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC₅₀= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer.

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Topoisomerase I/II inhibitor 2 Chemical Structure

CAS No. : 2770804-58-3

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Topoisomerase Topo I Topo II

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Topoisomerase I

Topoisomerase II

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	36.3 μM Compound: 1a	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 34802836]
BGC-823	IC₅₀	17.7 μM Compound: 1a	Antiproliferative activity against human BGC-823 cells after 72 hrs by MTT assay Antiproliferative activity against human BGC-823 cells after 72 hrs by MTT assay	[PMID: 34802836]
HCCLM9	IC₅₀	6.83 μM Compound: 1a	Antiproliferative activity against human HCCLM9 cells after 72 hrs by MTT assay Antiproliferative activity against human HCCLM9 cells after 72 hrs by MTT assay	[PMID: 34802836]
HCT-116	IC₅₀	64 μM Compound: 1a	Antiproliferative activity against human HCT-116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells after 72 hrs by MTT assay	[PMID: 34802836]
HepG2	IC₅₀	52 μM Compound: 1a	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 34802836]
HGC-27	IC₅₀	34.25 μM Compound: 1a	Antiproliferative activity against human HGC-27 cells after 72 hrs by MTT assay Antiproliferative activity against human HGC-27 cells after 72 hrs by MTT assay	[PMID: 34802836]
HL-60	IC₅₀	59.14 μM Compound: 1a	Antiproliferative activity against human HL-60 cells after 72 hrs by MTT assay Antiproliferative activity against human HL-60 cells after 72 hrs by MTT assay	[PMID: 34802836]
HT-29	IC₅₀	31 μM Compound: 1a	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 34802836]
Huh-7	IC₅₀	9.82 μM Compound: 1a	Antiproliferative activity against human Huh-7 cells after 72 hrs by MTT assay Antiproliferative activity against human Huh-7 cells after 72 hrs by MTT assay	[PMID: 34802836]
L02	IC₅₀	> 150 μM Compound: 1a	Antiproliferative activity against human L02 cells after 72 hrs by MTT assay Antiproliferative activity against human L02 cells after 72 hrs by MTT assay	[PMID: 34802836]
MCF7	IC₅₀	22.4 μM Compound: 1a	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 34802836]
MDA-MB-231	IC₅₀	19.9 μM Compound: 1a	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 34802836]
RKO	IC₅₀	47.8 μM Compound: 1a	Antiproliferative activity against human RKO cells after 72 hrs by MTT assay Antiproliferative activity against human RKO cells after 72 hrs by MTT assay	[PMID: 34802836]
SGC-7901	IC₅₀	30.76 μM Compound: 1a	Antiproliferative activity against human SGC-7901 cells after 72 hrs by MTT assay Antiproliferative activity against human SGC-7901 cells after 72 hrs by MTT assay	[PMID: 34802836]
SK-HEP1	IC₅₀	16.53 μM Compound: 1a	Antiproliferative activity against human SK-HEP1 cells after 72 hrs by MTT assay Antiproliferative activity against human SK-HEP1 cells after 72 hrs by MTT assay	[PMID: 34802836]
SW480	IC₅₀	9.04 μM Compound: 1a	Antiproliferative activity against human SW480 cells after 72 hrs by MTT assay Antiproliferative activity against human SW480 cells after 72 hrs by MTT assay	[PMID: 34802836]
U-251	IC₅₀	13.5 μM Compound: 1a	Antiproliferative activity against human U-251 cells after 72 hrs by MTT assay Antiproliferative activity against human U-251 cells after 72 hrs by MTT assay	[PMID: 34802836]

In Vitro

Topoisomerase I/II inhibitor 2 (compound 1a) (0-150 μM; 72 hours) has favourable anti-proliferative activity in cancer cell lines, and better inhibitory activity on two human hepatocellular carcinoma cell lines (HuH7, LM9)^[1].
Topoisomerase I/II inhibitor 2 (20 μM; 24 hours) has no damage to the DNA of HuH7 cells while some damage is noticed on LM9 cells^[1].
Topoisomerase I/II inhibitor 2 (1.25-8 μM; 1-2 weeks) inhibits cell proliferation of LM9 and Huh7 in a concentration-dependent manner^[1].
Topoisomerase I/II inhibitor 2 (1.25-8 μM; 24 hours) has a good inhibitory effect on the migration and invasion of LM9 and HuH7 cells with concentration-dependent manner^[1].
Topoisomerase I/II inhibitor 2 (0-20 μM; 24 hours) can inhibit the expression of matrix metalloproteinases-9 (MMP-9) in LM9 and HuH7 cells^[1].
Topoisomerase I/II inhibitor 2 (0-20 μM; 48 hours) inhibits cells proliferation by blocking cell cycle at the G₂/M phase^[1].
Topoisomerase I/II inhibitor 2 (3.5-20 μM; 48 hours) can injure mitochondrial function and induce cell apoptosis in a concentration-dependent manner^[1].

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

Cell Proliferation Assay

Cell Line:	LM9, HuH7, SK-hep-1, HepG2, HT-29, HCT-116, RKO, SW480, MCF-7, MDA-B-231, HGC-27, SGC-7901, BGC-823, A549, U251, HL-60, LO2^[1]
Concentration:	0-150 μM
Incubation Time:	72 hours
Result:	Displayed favourable anti-proliferative activity and had better inhibitory activity on two human hepatocellular carcinoma cell lines (HuH7, LM9).

Western Blot Analysis

Cell Line:	LM9 and HuH7 cells^[1]
Concentration:	0, 3.75, 7.5, 15 μM in LM9; 0, 5, 10, 20 μM in HuH7
Incubation Time:	48 hours
Result:	Inhibited the expression of MMP-9.

Cell Cycle Analysis

Cell Line:	LM9 and HuH7 cells^[1]
Concentration:	0, 3.75, 7.5, 15 μM in LM9; 0, 5, 10, 20 μM in HuH7
Incubation Time:	48 hours
Result:	Inhibited cells proliferation by blocking cell cycle at the G₂/M phase.

Apoptosis Analysis

Cell Line:	LM9 and HuH7 cells^[1]
Concentration:	3.5, 7, 14 μM in LM9; 5, 10, 20 μM in HuH7
Incubation Time:	48 hours
Result:	Induced apoptosis in a dose-dependent manner.

Molecular Weight

336.34

Formula

C₁₉H₁₆N₂O₄

CAS No.

2770804-58-3

SMILES

CNCC1=CC2=C(OCO2)C=C1C3=CC4=C(C5=C(OCO5)C=C4)C=N3

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, et al. Design, synthesis and anti-hepatocellular carcinoma activity of 3-arylisoquinoline alkaloids. Eur J Med Chem. 2022;228:113985. [Content Brief]