标签归档：topoisomerase

Topoisomerase I inhibitor 7

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Topoisomerase I inhibitor 7 

Topoisomerase I inhibitor 7 (Compound 8) 是一种有效的 Topoisomerase I 抑制剂。Topoisomerase I inhibitor 7 显着抑制肿瘤生长（高达 79%）并延长接受 P388 淋巴瘤移植的小鼠的寿命（153%）。Topoisomerase I inhibitor 7 表明了在杂芳烃融合蒽醌类中进一步寻找新的抗肿瘤候选药物的前景。

Topoisomerase I inhibitor 7

Topoisomerase I inhibitor 7 Chemical Structure

CAS No. : 2408639-81-4

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生物活性

Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants. Topoisomerase I inhibitor 7 indicates prospects for further search of new antitumor drug candidates among the heteroarene-fused anthraquinones[1].

分子量

405.40

Formula

C22H19N3O5
CAS 号

2408639-81-4
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.
参考文献

  • [1]. Tikhomirov AS, et al. Amides of pyrrole- and thiophene-fused anthraquinone derivatives: A role of the heterocyclic core in antitumor properties. Eur J Med Chem. 2020 Aug 1;199:112294.

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Topoisomerase II inhibitor 6

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Topoisomerase II inhibitor 6 

Topoisomerase II inhibitor 6 (Compound 5) 是一种色胺酮衍生物，是一种有效的、选择性的 topoisomerase II 抑制剂。Topoisomerase II inhibitor 6 对不同的肿瘤细胞系表现出抗增殖活性。Topoisomerase II inhibitor 6 在 G2 期阻断 CCRF-CEM 的细胞周期并诱导 DNA DSB。Topoisomerase II inhibitor 6 具有研究癌症疾病的潜力。

Topoisomerase II inhibitor 6

Topoisomerase II inhibitor 6 Chemical Structure

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生物活性

Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective inhibitor of topoisomerase II. Topoisomerase II inhibitor 6 exhibits antiproliferative activity on different tumor cell lines. Topoisomerase II inhibitor 6 blocks the cell cycle of CCRF-CEM in the G2 phase and induces DNA DSB. Topoisomerase II inhibitor 6 has the potential for the research of cancer diseases[1].

分子量

334.37

Formula

C19H18N4O2
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.
参考文献

  • [1]. Catanzaro E, et al. Targeting topoisomerase II with trypthantrin derivatives: Discovery of 7-((2-(dimethylamino)ethyl)amino)indolo[2,1-b]quinazoline-6,12-dione as an antiproliferative agent and to treat cancer. Eur J Med Chem. 2020 Sep 15;202:112504.

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Topoisomerase I inhibitor 6

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Topoisomerase I inhibitor 6 

Topoisomerase I inhibitor 6 (Compound 3) 是一种有效的 Topoisomerase I 抑制剂。Topoisomerase I inhibitor 6 能够捕获 DNA-Top1 裂解复合物，并被发现在非癌细胞系中的细胞毒性较小。Topoisomerase I inhibitor 6 具有研究癌症疾病的潜力。

Topoisomerase I inhibitor 6

Topoisomerase I inhibitor 6 Chemical Structure

CAS No. : 2393082-56-7

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生物活性

Topoisomerase I inhibitor 6 (Compound 3) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 6 is able to trap DNA-Top1 cleavage complex and found to be less cytotoxic in non-cancerous cell line. Topoisomerase I inhibitor 6 has the potential for the research of cancer diseases[1].

分子量

411.46

Formula

C23H21N7O
CAS 号

2393082-56-7
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.
参考文献

  • [1]. Kundu B, et al. Development of a metabolically stable topoisomerase I poison as anticancer agent. Eur J Med Chem. 2020 Sep 15;202:112551. doi: 10.1016/j.ejmech.2020.112551.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Topoisomerase I/II inhibitor 2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Topoisomerase I/II inhibitor 2 

Topoisomerase I/II inhibitor 2 (compound 1a) 是一种有效的拓扑异构酶 (Topoisomerase) 抑制剂，Huh7 与 LM9 细胞中的 IC50 分别为 9.82 μM 和 6.83 μM。Topoisomerase I/II inhibitor 2 对 DNA 拓扑异构酶 I/II 具有双重抑制，也能抑制小鼠模型中的异种移植肿瘤。Topoisomerase I/II inhibitor 2 具有治疗肝癌的潜在价值。

Topoisomerase I/II inhibitor 2

Topoisomerase I/II inhibitor 2 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

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 treating liver cancer[1].

IC50 & Target

Topoisomerase I

 

Topoisomerase II

 

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd 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.

分子量

336.34

Formula

C19H16N2O4
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.
参考文献

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

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Topoisomerase I/II inhibitor 2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Topoisomerase I/II inhibitor 2 

Topoisomerase I/II inhibitor 2 (compound 1a) 是一种有效的拓扑异构酶 (Topoisomerase) 抑制剂，Huh7 与 LM9 细胞中的 IC50 分别为 9.82 μM 和 6.83 μM。Topoisomerase I/II inhibitor 2 对 DNA 拓扑异构酶 I/II 具有双重抑制，也能抑制小鼠模型中的异种移植肿瘤。Topoisomerase I/II inhibitor 2 具有治疗肝癌的潜在价值。

Topoisomerase I/II inhibitor 2

Topoisomerase I/II inhibitor 2 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

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 treating liver cancer[1].

IC50 & Target

Topoisomerase I

 

Topoisomerase II

 

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd 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.

分子量

336.34

Formula

C19H16N2O4
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.
参考文献

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

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Topoisomerase I/II inhibitor 2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Topoisomerase I/II inhibitor 2 

Topoisomerase I/II inhibitor 2 (compound 1a) 是一种有效的拓扑异构酶 (Topoisomerase) 抑制剂，Huh7 与 LM9 细胞中的 IC50 分别为 9.82 μM 和 6.83 μM。Topoisomerase I/II inhibitor 2 对 DNA 拓扑异构酶 I/II 具有双重抑制，也能抑制小鼠模型中的异种移植肿瘤。Topoisomerase I/II inhibitor 2 具有治疗肝癌的潜在价值。

Topoisomerase I/II inhibitor 2

Topoisomerase I/II inhibitor 2 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

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 treating liver cancer[1].

IC50 & Target

Topoisomerase I

 

Topoisomerase II

 

体外研究
(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].

上海金畔生物科技有限公司 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.

分子量

336.34

Formula

C19H16N2O4
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.
参考文献

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

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Topoisomerase I inhibitor 5

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Topoisomerase I inhibitor 5 

Topoisomerase I inhibitor 5 是一种有效的拓扑异构酶 (topoisomerase) 抑制剂。Topoisomerase I inhibitor 5 能干扰 DNA，显著抑制 Topoisomerase I 活性。Topoisomerase I inhibitor 5 能将细胞周期阻滞在 G1 期，诱导 MCF-7 细胞凋亡 (apoptosis)。Topoisomerase I inhibitor 5 具有逆转 P-gp 介导的阿霉素耐药性的效力。

Topoisomerase I inhibitor 5

Topoisomerase I inhibitor 5 Chemical Structure

CAS No. : 2513461-95-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin[1].

IC50 & Target

Topoisomerase I[1]
体外研究
(In Vitro)

Topoisomerase I inhibitor 5 (compound 14) (0-50 μM; 48 hours) exhibits antiproliferation activity against cancer cell lines and lower cytotoxicity in normal cells[1].
Topoisomerase I inhibitor 5 (2-8 μM; 24 hours) induces MCF-7 cell cycle arrest at the G1 phase[1].
Topoisomerase I inhibitor 5 (2-8 μM; 48 hours) increases the apoptotic rate of MCF-7/ADR and MCF-7 cells[1].
Topoisomerase I inhibitor 5 (1.5-6 μM; 24 hours) increases the expression degree of cleaved-caspase-3 and cleaved-PARP in MCF-7; down-regulates the level of anti-apoptotic protein, up-regulates the levels of pro-apoptotic proteins in MCF-7/ADR[1].
Topoisomerase I inhibitor 5 (0.1 μM; 24 hours) induces cell apoptosis by promoting the accumulation of ROS in MCF-7/ADR cell[1].
Topoisomerase I inhibitor 5 (10 μg/ml; 24 hours) increases the accumulation of the ADR and Rh123 in MCF-7/ADR cells[1].
Topoisomerase I inhibitor 5 (5, 10 and 20 μM; 24 hours) reduces the expression degree of P-gp by 14.95% and 18.10% in MCF-7/ADR cells at 10 and 20 μM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: A549, HepG-2, MCF-7, MDA-MB-231, MCF-7/ADR and LO2 cells[1]
Concentration: 0-50 μM
Incubation Time: 48 hours
Result: Exhibited antiproliferation activity against cancer cell lines, with IC50s of 2.39 ± 0.23 μM, 4.88 ± 0.29 μM, 1.32 ± 0.14 μM, 7.64 ± 0.35 μM and 2.42 ± 0.14 μM in A549, HepG-2, MCF-7, MDA-MB-231, MCF-7/ADR, respectively; and has lower cytotoxicity in LO2 cells with IC50 of 36.52 ± 2.36 μM.

Cell Cycle Analysis

Cell Line: MCF-7[1]
Concentration: 2, 4 and 8 μM
Incubation Time: 24 hours
Result: Induced MCF-7 cell cycle arrest at the G1 phase.

Apoptosis Analysis

Cell Line: MCF-7 and MCF-7/ADR cells[1]
Concentration: 2, 4 and 8 μM
Incubation Time: 48 hours
Result: Induced apoptosis in a dose-dependent manner in MCF-7 cells, and increased the apoptotic rate of the cells from 2.8% to 15.2% in MCF-7/ADR.

Western Blot Analysis

Cell Line: MCF-7[1]
Concentration: 1.5, 3 and 6 μM in MCF-7; 5, 10, and 20 μM in MCF-7/ADR
Incubation Time: 24 hours
Result: Increased the expression degree of cleaved-caspase-3 and cleaved-PARP in MCF-7; down-regulated the level of anti-apoptotic protein bcl-2, up-regulated the levels of pro-apoptotic proteins bax and bad in MCF-7/ADR.

体内研究
(In Vivo)

Topoisomerase I inhibitor 5 (1 mg/kg and 10 mg/kg; IV; every two days, for 21 days) decreases the tumor growth significantly[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Bal b/c nude mice (injected with 106 MCF-7 cells in the left flank for 7 days)[1]
Dosage: 1 mg/kg and 10 mg/kg
Administration: IV; every two days, for 21 days
Result: Decreased the tumor growth significantly and the tumor inhibition ratio reached to 32.4% at 1 mg/kg and 7.2% at 10 mg/kg.

分子量

372.46

Formula

C24H24N2O2
CAS 号

2513461-95-3
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.
参考文献

  • [1]. Zhong H, Zhao M, Wu C, Zhang J, Chen L, Sun J. Development of oxoisoaporphine derivatives with topoisomerase I inhibition and reversal of multidrug resistance in breast cancer MCF-7/ADR cells. Eur J Med Chem. 2022;235:114300.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Topoisomerase I inhibitor 5

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Topoisomerase I inhibitor 5 

Topoisomerase I inhibitor 5 是一种有效的拓扑异构酶 (topoisomerase) 抑制剂。Topoisomerase I inhibitor 5 能干扰 DNA，显著抑制 Topoisomerase I 活性。Topoisomerase I inhibitor 5 能将细胞周期阻滞在 G1 期，诱导 MCF-7 细胞凋亡 (apoptosis)。Topoisomerase I inhibitor 5 具有逆转 P-gp 介导的阿霉素耐药性的效力。

Topoisomerase I inhibitor 5

Topoisomerase I inhibitor 5 Chemical Structure

CAS No. : 2513461-95-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin[1].

IC50 & Target

Topoisomerase I[1]
体外研究
(In Vitro)

Topoisomerase I inhibitor 5 (compound 14) (0-50 μM; 48 hours) exhibits antiproliferation activity against cancer cell lines and lower cytotoxicity in normal cells[1].
Topoisomerase I inhibitor 5 (2-8 μM; 24 hours) induces MCF-7 cell cycle arrest at the G1 phase[1].
Topoisomerase I inhibitor 5 (2-8 μM; 48 hours) increases the apoptotic rate of MCF-7/ADR and MCF-7 cells[1].
Topoisomerase I inhibitor 5 (1.5-6 μM; 24 hours) increases the expression degree of cleaved-caspase-3 and cleaved-PARP in MCF-7; down-regulates the level of anti-apoptotic protein, up-regulates the levels of pro-apoptotic proteins in MCF-7/ADR[1].
Topoisomerase I inhibitor 5 (0.1 μM; 24 hours) induces cell apoptosis by promoting the accumulation of ROS in MCF-7/ADR cell[1].
Topoisomerase I inhibitor 5 (10 μg/ml; 24 hours) increases the accumulation of the ADR and Rh123 in MCF-7/ADR cells[1].
Topoisomerase I inhibitor 5 (5, 10 and 20 μM; 24 hours) reduces the expression degree of P-gp by 14.95% and 18.10% in MCF-7/ADR cells at 10 and 20 μM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: A549, HepG-2, MCF-7, MDA-MB-231, MCF-7/ADR and LO2 cells[1]
Concentration: 0-50 μM
Incubation Time: 48 hours
Result: Exhibited antiproliferation activity against cancer cell lines, with IC50s of 2.39 ± 0.23 μM, 4.88 ± 0.29 μM, 1.32 ± 0.14 μM, 7.64 ± 0.35 μM and 2.42 ± 0.14 μM in A549, HepG-2, MCF-7, MDA-MB-231, MCF-7/ADR, respectively; and has lower cytotoxicity in LO2 cells with IC50 of 36.52 ± 2.36 μM.

Cell Cycle Analysis

Cell Line: MCF-7[1]
Concentration: 2, 4 and 8 μM
Incubation Time: 24 hours
Result: Induced MCF-7 cell cycle arrest at the G1 phase.

Apoptosis Analysis

Cell Line: MCF-7 and MCF-7/ADR cells[1]
Concentration: 2, 4 and 8 μM
Incubation Time: 48 hours
Result: Induced apoptosis in a dose-dependent manner in MCF-7 cells, and increased the apoptotic rate of the cells from 2.8% to 15.2% in MCF-7/ADR.

Western Blot Analysis

Cell Line: MCF-7[1]
Concentration: 1.5, 3 and 6 μM in MCF-7; 5, 10, and 20 μM in MCF-7/ADR
Incubation Time: 24 hours
Result: Increased the expression degree of cleaved-caspase-3 and cleaved-PARP in MCF-7; down-regulated the level of anti-apoptotic protein bcl-2, up-regulated the levels of pro-apoptotic proteins bax and bad in MCF-7/ADR.

体内研究
(In Vivo)

Topoisomerase I inhibitor 5 (1 mg/kg and 10 mg/kg; IV; every two days, for 21 days) decreases the tumor growth significantly[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Bal b/c nude mice (injected with 106 MCF-7 cells in the left flank for 7 days)[1]
Dosage: 1 mg/kg and 10 mg/kg
Administration: IV; every two days, for 21 days
Result: Decreased the tumor growth significantly and the tumor inhibition ratio reached to 32.4% at 1 mg/kg and 7.2% at 10 mg/kg.

分子量

372.46

Formula

C24H24N2O2
CAS 号

2513461-95-3
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.
参考文献

  • [1]. Zhong H, Zhao M, Wu C, Zhang J, Chen L, Sun J. Development of oxoisoaporphine derivatives with topoisomerase I inhibition and reversal of multidrug resistance in breast cancer MCF-7/ADR cells. Eur J Med Chem. 2022;235:114300.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Topoisomerase I inhibitor 5

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Topoisomerase I inhibitor 5 

Topoisomerase I inhibitor 5 是一种有效的拓扑异构酶 (topoisomerase) 抑制剂。Topoisomerase I inhibitor 5 能干扰 DNA，显著抑制 Topoisomerase I 活性。Topoisomerase I inhibitor 5 能将细胞周期阻滞在 G1 期，诱导 MCF-7 细胞凋亡 (apoptosis)。Topoisomerase I inhibitor 5 具有逆转 P-gp 介导的阿霉素耐药性的效力。

Topoisomerase I inhibitor 5

Topoisomerase I inhibitor 5 Chemical Structure

CAS No. : 2513461-95-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin[1].

IC50 & Target

Topoisomerase I[1]
体外研究
(In Vitro)

Topoisomerase I inhibitor 5 (compound 14) (0-50 μM; 48 hours) exhibits antiproliferation activity against cancer cell lines and lower cytotoxicity in normal cells[1].
Topoisomerase I inhibitor 5 (2-8 μM; 24 hours) induces MCF-7 cell cycle arrest at the G1 phase[1].
Topoisomerase I inhibitor 5 (2-8 μM; 48 hours) increases the apoptotic rate of MCF-7/ADR and MCF-7 cells[1].
Topoisomerase I inhibitor 5 (1.5-6 μM; 24 hours) increases the expression degree of cleaved-caspase-3 and cleaved-PARP in MCF-7; down-regulates the level of anti-apoptotic protein, up-regulates the levels of pro-apoptotic proteins in MCF-7/ADR[1].
Topoisomerase I inhibitor 5 (0.1 μM; 24 hours) induces cell apoptosis by promoting the accumulation of ROS in MCF-7/ADR cell[1].
Topoisomerase I inhibitor 5 (10 μg/ml; 24 hours) increases the accumulation of the ADR and Rh123 in MCF-7/ADR cells[1].
Topoisomerase I inhibitor 5 (5, 10 and 20 μM; 24 hours) reduces the expression degree of P-gp by 14.95% and 18.10% in MCF-7/ADR cells at 10 and 20 μM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: A549, HepG-2, MCF-7, MDA-MB-231, MCF-7/ADR and LO2 cells[1]
Concentration: 0-50 μM
Incubation Time: 48 hours
Result: Exhibited antiproliferation activity against cancer cell lines, with IC50s of 2.39 ± 0.23 μM, 4.88 ± 0.29 μM, 1.32 ± 0.14 μM, 7.64 ± 0.35 μM and 2.42 ± 0.14 μM in A549, HepG-2, MCF-7, MDA-MB-231, MCF-7/ADR, respectively; and has lower cytotoxicity in LO2 cells with IC50 of 36.52 ± 2.36 μM.

Cell Cycle Analysis

Cell Line: MCF-7[1]
Concentration: 2, 4 and 8 μM
Incubation Time: 24 hours
Result: Induced MCF-7 cell cycle arrest at the G1 phase.

Apoptosis Analysis

Cell Line: MCF-7 and MCF-7/ADR cells[1]
Concentration: 2, 4 and 8 μM
Incubation Time: 48 hours
Result: Induced apoptosis in a dose-dependent manner in MCF-7 cells, and increased the apoptotic rate of the cells from 2.8% to 15.2% in MCF-7/ADR.

Western Blot Analysis

Cell Line: MCF-7[1]
Concentration: 1.5, 3 and 6 μM in MCF-7; 5, 10, and 20 μM in MCF-7/ADR
Incubation Time: 24 hours
Result: Increased the expression degree of cleaved-caspase-3 and cleaved-PARP in MCF-7; down-regulated the level of anti-apoptotic protein bcl-2, up-regulated the levels of pro-apoptotic proteins bax and bad in MCF-7/ADR.

体内研究
(In Vivo)

Topoisomerase I inhibitor 5 (1 mg/kg and 10 mg/kg; IV; every two days, for 21 days) decreases the tumor growth significantly[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Bal b/c nude mice (injected with 106 MCF-7 cells in the left flank for 7 days)[1]
Dosage: 1 mg/kg and 10 mg/kg
Administration: IV; every two days, for 21 days
Result: Decreased the tumor growth significantly and the tumor inhibition ratio reached to 32.4% at 1 mg/kg and 7.2% at 10 mg/kg.

分子量

372.46

Formula

C24H24N2O2
CAS 号

2513461-95-3
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.
参考文献

  • [1]. Zhong H, Zhao M, Wu C, Zhang J, Chen L, Sun J. Development of oxoisoaporphine derivatives with topoisomerase I inhibition and reversal of multidrug resistance in breast cancer MCF-7/ADR cells. Eur J Med Chem. 2022;235:114300.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Topoisomerase I/II inhibitor 3

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Topoisomerase I/II inhibitor 3 

Topoisomerase I/II inhibitor 3 (7) 是一种有效的拓扑异构酶 I (Topo I) 和 II (Topo II) 双抑制剂。Topoisomerase I/II inhibitor 3 通过抑制 PI3K/Akt/mTOR 信号通路抑制细胞增殖、侵袭和迁移，诱导细胞凋亡(apoptosis)。Topoisomerase I/II inhibitor 3 可用于肝癌的研究。

Topoisomerase I/II inhibitor 3

Topoisomerase I/II inhibitor 3 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

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[1].

IC50 & Target

Topoisomerase I

 

Topoisomerase II

 

PI3K

 

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd 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.

体内研究
(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].

Shanghai Jinpan Biotech Co Ltd 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.

分子量

404.46

Formula

C24H24N2O4
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.
参考文献

  • [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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务