Topoisomerase IIα-IN-5

製品番号: HY-152187: Data Sheet 取扱説明書
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Topoisomerase IIα-IN-5 is a topoisomerase II (topo II) α catalytic inhibitor. Topoisomerase IIα-IN-5 intercalates into DNA and binds to the DNA minor groove. Topoisomerase IIα-IN-5 exhibits better efficacy and less genotoxicity than Etoposide (HY-13629).

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Topoisomerase IIα-IN-5 構造式

CAS 番号 : 3037545-23-3

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Topoisomerase Topo I Topo II DNA gyrase

生物活性
純度とドキュメンテーション
参考文献
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製品説明

IC₅₀ & Target^[1]

topoisomerase II alpha

Cellular Effect

Cell Line	Type	Value	Description	References
DU-145	IC₅₀	0.13 μM Compound: 6	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell proliferation incubated for 72 hrs by WST assay Antiproliferative activity against human DU-145 cells assessed as inhibition of cell proliferation incubated for 72 hrs by WST assay	[PMID: 36493620]
HCT-15	IC₅₀	9.25 μM Compound: 6	Antiproliferative activity against human HCT-15 cells assessed as inhibition of cell proliferation incubated for 72 hrs by WST assay Antiproliferative activity against human HCT-15 cells assessed as inhibition of cell proliferation incubated for 72 hrs by WST assay	[PMID: 36493620]
T47D	IC₅₀	0.53 μM Compound: 6	Antiproliferative activity against human T47D cells assessed as inhibition of cell proliferation incubated for 72 hrs by WST assay Antiproliferative activity against human T47D cells assessed as inhibition of cell proliferation incubated for 72 hrs by WST assay	[PMID: 36493620]

体外実験

Topoisomerase IIα-IN-5 (compound 6) (5 μM, 10 μM, and 20 μM; 10 d) inhibits colony formation of DU145 cells^[1].
Topoisomerase IIα-IN-5 (1 μM and 10 μM; 72 h) shows antiproliferative against DU145 cells^[1].
Topoisomerase IIα-IN-5 has cytotoxicity against DU145, HCT15, and T47D cells with IC₅₀s of 0.13 μM, 9.25 μM, and 0.53 μM, respectively^[1].
Topoisomerase IIα-IN-5 (200 μM) interacts with a DNA double helix^[1].
Topoisomerase IIα-IN-5 (20 μM; 24 h) induces G2 cell cycle arrest and apoptosis in CRPC cells^[1].

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

Western Blot Analysis^[1]

Cell Line:	CRPC cells
Concentration:	0, 5, 10, and 20 μM
Incubation Time:	0, 8, 16, and 24 hours
Result:	Increased the expression of both phosphorylated cdc25c and phosphorylated cdc2.

Apoptosis Analysis^[1]

Cell Line:	CRPC cells
Concentration:	0, 5, 10, and 20 μM
Incubation Time:	0, 8, 16, and 24 hours
Result:	Induced cell cycle arrest at G2 phase. Induced cell apoptosis.

分子量

438.52

分子式

C₂₅H₃₀N₂O₅

CAS 番号

3037545-23-3

SMILES

O=C1C=C(OC2=CC(OCC(CNCCN3CCCCC3)O)=CC(O)=C12)C4=CC=CC=C4

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Jeon KH, et al. Synthesis and evaluation of 7-(3-aminopropyloxy)-substituted flavone analogue as a topoisomerase IIα catalytic inhibitor and its sensitizing effect to enzalutamide in castration-resistant prostate cancer cells. Eur J Med Chem. 2023 Jan 15;246:114999. [Content Brief]