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Cat. No.: HY-151453

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Topoisomerase IIα-IN-4

Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC₅₀ value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer.

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

CAS No.: 2860554-26-1
Formula: C₂₅H₂₁NO₂
Molecular Weight:367.44

Storage:

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

Data Sheet (271 KB)

Topoisomerase IIα-IN-4 Chemical Structure

CAS No.: 2860554-26-1

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

topoisomerase II alpha

3.8 μM (IC₅₀)

topoisomerase II beta

10.1 μM (IC₅₀)

All Topoisomerase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.3 μM Compound: F2	Antiproliferative activity against human A549 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells incubated for 72 hrs by CCK8 assay	[PMID: 36063665]
BEAS-2B	IC₅₀	31.9 μM Compound: F2	Antiproliferative activity against human BEAS-2B cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human BEAS-2B cells incubated for 72 hrs by CCK8 assay	[PMID: 36063665]
HCT-116	IC₅₀	0.2 μM Compound: F2	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by CCK8 assay	[PMID: 36063665]
HeLa	IC₅₀	0.1 μM Compound: F2	Antiproliferative activity against human HeLa cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HeLa cells incubated for 72 hrs by CCK8 assay	[PMID: 36063665]
HepG2	IC₅₀	0.3 μM Compound: F2	Antiproliferative activity against human HepG2 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells incubated for 72 hrs by CCK8 assay	[PMID: 36063665]
L02	IC₅₀	16.7 μM Compound: F2	Antiproliferative activity against human HL7702 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HL7702 cells incubated for 72 hrs by CCK8 assay	[PMID: 36063665]
MDA-MB-231	IC₅₀	0.2 μM Compound: F2	Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CCK8 assay	[PMID: 36063665]
PC-3	IC₅₀	0.3 μM Compound: F2	Antiproliferative activity against human PC-3 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human PC-3 cells incubated for 72 hrs by CCK8 assay	[PMID: 36063665]

In Vitro

Topoisomerase IIα-IN-4 (0-50 μM; 72 h) shows antiproliferative activities against cancer cells^[1].
Topoisomerase IIα-IN-4 shows high inhibitory activity and subtypeselectivity against TopoIIα and β with IC₅₀s of 3.8 and 10.1 μM, respectively^[1].
Topoisomerase IIα-IN-4 (0.3 μM; 4 h) is a non-intercalative TopoIIα catalytic inhibitor^[1].
Topoisomerase IIα-IN-4 (0.5-1 μM; 48 h) induces cell apoptosis^[1].
Topoisomerase IIα-IN-4 (0.5-1 μM; 24 h) induces cell-cycle arrest^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

HeLa, HCT-116, MDA-MB231, HepG2, A549, CCL-226, BEAS-2B and HL-7702 cell lines
Concentration:

0-50 μM
Incubation Time:

72 hours
Result:

Inhibited HeLa, HCT-116, MDA-MB 231, HepG2, A549, CCL-226, BEAS-2B and HL-7702 cells with IC₅₀s of 0.1, 0.2, 0.3, 0.2, 0.3, 0.3, ＞50, 31.9 and 16.7 μM, respectively.

Western Blot Analysis^[1]

Cell Line:

HepG-2 cell line
Concentration:

0.3 μM
Incubation Time:

4 hours
Result:

Showed no effect on the level of phospho-histone H2AX.

Apoptosis Analysis^[1]

Cell Line:

0.5-1 μM
Concentration:

0.3 μM
Incubation Time:

48 hours
Result:

Increased the total numbers of early and late apoptotic cells from 6.0% to 70.6% at the concentration of 1 μM.

In Vivo

Topoisomerase IIα-IN-4 (500 mg/kg; p.o. twice at the first day) shows no acute toxicity in vivo^[1].

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

Animal Model:

C57BL/6 mice^[1]
Dosage:

500 mg/kg
Administration:

Oral gavage; 500 mg/kg twice at the first day
Result:

Exerted lower toxicity in this established test and caused no significant difference of body weight of mice.

Chemical Information

CAS No. 2860554-26-1
Molecular Weight 367.44
Formula C₂₅H₂₁NO₂
SMILES

O=C(NC1=CC=C(C2=CC=C3C=C(O)C=CC3=C2)C=C1)CCC4=CC=CC=C4
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Xu G, et al. Discovery of 1,2-diphenylethene derivatives as human DNA topoisomerase II catalytic inhibitors and antitumor agents. Eur J Med Chem. 2022 Aug 26;243:114706. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Topoisomerase IIα-IN-4

All Topoisomerase Isoforms