2. Cell Cycle/DNA Damage Apoptosis
  3. Topoisomerase Apoptosis MDM-2/p53 Bcl-2 Family Caspase
  4. Topoisomerase I/II-IN-1

Topoisomerase I/II-IN-1 是 Topoisomerase I/II 的双重抑制剂。Topoisomerase I/II-IN-1 通过上调 p53、p21、Bax mRNA 水平、caspase-3 蛋白水平和 Bax/Bcl-2 比例，并下调 Bcl-2，诱导癌细胞 G2/M 停滞和凋亡 (apoptosis)。Topoisomerase I/II-IN-1 可用于黑色素瘤、肾癌、肠癌、乳腺癌等多种癌症的研究。

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Topoisomerase I/II-IN-1 Chemical Structure

Topoisomerase I/II-IN-1 Chemical Structure

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Customer Review

Topoisomerase I/II-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Topoisomerase 亚型特异性产品:

查看所有亚型
Topoisomerase Topo I Topo II

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Topoisomerase I/II-IN-1 is a dual inhibitor of topoisomerase I/II. Topoisomerase I/II-IN-1 induces G2/M arrest and apoptosis in cancer cells by upregulating p53, p21, and Bax mRNA levels, caspase-3 protein levels, and the Bax/Bcl-2 ratio, while downregulating Bcl-2. Topoisomerase I/II-IN-1 is useful in the study of various cancers, including melanoma, renal cancer, colorectal cancer, and breast cancer[1].

IC50 & Target[1]

Topoisomerase I

 

Topoisomerase II

 

Caspase 3

 

体外研究
(In Vitro)

Topoisomerase I/II-IN-1 (Compound 5j) (10 μM)对多种癌细胞表现出抑制作用：对黑色素瘤 LOX IMVI 细胞的生长抑制率 (GI) 为 -93.46%，对结直肠癌 HCT-116、HCT-15 和 SW-620 细胞的 GI 分别为 -59.51%、-40.12% 和 -43.01%，对乳腺癌细胞 MDA-MB-468 的 GI 为 -24.45%，对肾癌细胞 786-0、RXF 393 和 UO-31 的 GI 分别为 -11.21%、-12.44% 和 -29.74%[1]。

Topoisomerase I/II-IN-1 抑制 Topo I/Topo IIβ 酶活性，在 LOX IMVI 细胞系中的抑制率分别为61.58%/75.51%，在 HCT-116 结肠癌中的抑制率分别为 56.42%/76.39%[1]。

Topoisomerase I/II-IN-1 (24小时) 通过上调 HCT-116 和 LOX IMVI 细胞中的 p53、p21、Bax mRNA 水平、裂解的 caspase-3 蛋白水平和 Bax/Bcl-2 比例，并下调 Bcl-2，诱导癌细胞 G2/M 停滞和凋亡[1]。

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

Topoisomerase I/II-IN-1 相关抗体:

Cell Cycle Analysis[1]

Cell Line: HCT-116 and LOX IMVI cells
Concentration: /
Incubation Time: 24 h
Result: Increased the percentage of cells in pre-G1 phase to 34.27%, upregulated the percentage of cells in G2/M phase to 33.32%, and decreased the percentage of cells in S phase to 29.17% in HCT116 cells.
Increased the proportion of cells in the G2/M phase to 27.54%, and decreased the percentage of cells in the S phase to 28.58% in LOX IMVI cells.

Apoptosis Analysis[1]

Cell Line: HCT-116 and LOX IMVI cells
Concentration: /
Incubation Time: 24 h
Result: Decreased the survival rate, which was 0.43% and 0.42%, respectively, and increased the number of necrotic cells, which was 9.22% and 4.88%, respectively, but the number of apoptotic cells was still higher than that of necrotic cells, which was 34.27% and 36.85%, respectively.
分子量

614.62

Formula

C33H31FN4O7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Topoisomerase I/II-IN-1 相关分类

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  • 稀释计算器

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Help & FAQs
  • 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.

Keywords:

Topoisomerase I/II-IN-1TopoisomeraseApoptosisMDM-2/p53Bcl-2 FamilyCaspaseInhibitorHCT-116 cellsLOX IMVI cellsMelanomaKidney cancerColorectal cancerBreast cancerinhibitorinhibit

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