Topoisomerase

XR-11576 is a DNA topoisomerase I and II inhibitor for the treatment of solid tumors.

RPR121056 is a Irinotecan metabolite, which is generated by CYP3A4. Irinotecan is an antineoplastic agent that inhibits topoisomerase type I.

Gepotidacin mesylate dihydrate (GSK2140944 mesylate dihydrate) 是一种可口服的三氮杂苊烯抗生素，具有抗菌活性。Gepotidacin mesylate dihydrate 是细菌 II 型拓扑异构酶抑制剂。Gepotidacin mesylate dihydrate 通过阻断拓扑异构酶来抑制细菌 DNA 复制，可用于研究细菌感染。

7Ethanol-10NH2-11F-Camptothecin 是一抗体-活性分子偶联物(ADC)，具有抑制肿瘤生长的功能，适用于癌症研究。

Intoplicine is an inhibitor of DNA topoisomerase I and II.

Anticancer agent 75 具有良好的抗疟原虫活性。Anticancer agent 75 是有效的抗癌剂，在癌细胞系中表现出细胞毒性和选择性。Anticancer agent 75 对正常人肾细胞系的细胞毒性比阿霉素标准品至少低 35 倍。

Exatecan Mesylate (DX8951f) 是一种 DNA 拓扑异构酶 I 抑制剂，IC50值为 2.2 μM，可研究癌症。

Irinotecan hydrochloride trihydrate (CPT-11 HCl Trihydrate) 通过抑制拓扑异构酶 1 来防止 DNA 展开，可研究结肠癌和直肠癌。

Topoisomerase II inhibitor 11 (compound 3d) 是一种拓扑异构酶 II (Topoisomerase II) 的有效抑制剂 (IC50: 2.89 μM)。Topoisomerase II inhibitor 11 对肾癌 A498 细胞有 92.46% 的抑制效果 (IC50: 3.5 μM)。Topoisomerase II inhibitor 11 能够将细胞周期阻滞在 G2/M 期，抑制细胞增殖并具有凋亡活性。

Rebeccamycin is an antitumor antibiotic+ inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I. It also has a negligible effect on protein kinase C and topoisomerase II.

Berberine (Umbellatine) 属于生物碱类天然产物，可以激活 AMPK、抑制 DNA 拓扑异构酶、诱导 ROS 生成。Berberine 具有抗肿瘤、抗菌、降血糖、降血脂等生物学活性。

Trovafloxacin 是广谱喹诺酮类抗生素，对革兰氏阳性，革兰氏阴性和厌氧菌有活性。它可阻断 DNA 促旋酶 和拓扑异构酶 IV 的活性。它也是口服活性的 Pannexin 1通道选择性抑制剂，对 PANX1内向电流的 IC50为 4 μM。

Banoxantrone D12 (AQ4N D12) is the deuterium-labeled form of Banoxantrone, a bioreductive agent that can be metabolically converted to AQ4, a stable compound with DNA affinity and topoisomerase II inhibition properties.

Podocarpusflavone A 是一个 DNA topoisomerase I 和 STAT3 抑制剂，是从台湾特有植物罗汉果中分离出来的黄酮类化合物，具有潜在的抗利什曼原虫活性和抗肿瘤活性。Podocarpusflavone A，抑制皮肤皮肤黑色素瘤的细胞生长。

Ledoxantrone trihydrochloride 是一种 Top II 抑制剂，具有抗癌活性，可用于研究消化系统疾病和泌尿系统疾病。

CAY10744 is a topoisomerase II-α poison.1 It inhibits topoisomerase II-α by 78.9% when used at a concentration of 20 μM. CAY10744 is selective for topoisomerase II-α over topoisomerase I providing 100 and 0% inhibition, respectively, at 100 μM. It inhibits proliferation of HCT15 colon, T47D breast, DU145 prostate, and HeLa cervical cancer cells (IC50s = 0.014, 0.00267, 0.072, and 2.46 μM, respectively). CAY10744 induces apoptosis in T47D cells when used at concentrations of 10 and 30 μM. CAY10744 (12 mg/kg per day) reduces tumor growth in an MDA-MB-231 orthotopic mouse model of breast cancer. |1. Kadayat, T.M., Park, S., Shrestha, A., et al. Discovery and biological evaluations of halogenated 2,4-diphenyl indeno[1,2-b]pyridinol derivatives as potent topoisomerase IIa-targeted chemotherapeutic agents for breast cancer. J. Med. Chem. 62, 8194-8234 (2019).

Karenitecin (Cositecan) is an inhibitor of topoisomerase I. It has potent anti-cancer activity.

Mauritianin 是一种从 Acalypha indica 的花和叶中分离出来的山柰酚苷，是一种拓扑异构酶 I 抑制剂。Mauritianin 具有细胞保护活性。

TAS-103 dihydrochloride (BMS-247615 dihydrochloride) 是可用于癌症研究的一种 DNA 拓扑异构酶 I/II 双重抑制剂。

Pirarubicin (Theprubicin) 是一种蒽环类抗生素，是拓扑异构酶 II 抑制剂，可用于各种癌症的研究。

5,7,3',5'-tetrahydroxy-6,4'-dimethoxyflavone exhibits anti-HIV-1 activity in the anti-syncytium assay using (∆Tat/rev)MC99 virus and 1A2 cell line system, it shows considerably activity against HIV-1 reverse transcriptase. It exhibits cytotoxic activity against P-388 cell lines, it can inhibit DNA topoisomerase IIα activity, which may be responsible for the observed cytotoxicity.

Sutopin-2 是一种拓扑异构酶 II 抑制剂。它影响细胞周期进程及微管的稳定性，并通过调节细胞核-细胞质转运的细胞周期蛋白 B1 诱导细胞周期停滞。

(1S,2R,7S)-Sitafloxacin (DU-6856) 是 Sitafloxacin 的对映异构体，它作为拓扑异构酶抑制剂及抗生素，对大肠杆菌 DNA 旋转酶 (IC50 0.18 μg/mL) 和金黄色葡萄球菌拓扑异构酶 IV 具有抑制活性，其抗菌特性适用于各种细菌感染的研究。

NC190 is an inhibitor of topoisomerase II that inhibited the growth of FM3A cells in clinical trials. NC-190 strongly inhibited the growth of FM3A cells when cultured with NC-190 for 48 h (IC50: 0.019 μg/ml). NC-190 potently suppressed DNA synthesis with

Hippeastrine hydrobromide is a natural alkaloid which demonstrates significant cytotoxicity against a panel of human and murine tumor cell lines.

Camptothecin-20(S)-O-propionate hydrate 作为Camptothecin的衍生物，属于强效抗肿瘤化合物。它主要通过抑制拓扑异构酶 I (topoisomerase-Ι) 来发挥作用。

SN-398 是一种 Camptothecin 衍生物，作为抗肿瘤药物，通过抑制哺乳动物 DNA 拓扑异构酶I (Topo I) 发挥作用。它通过稳定 Topo I-DNA 复合物来阻止 DNA 重新连接，从而诱导 Topo I 介导的 DNA 断裂。在 Hela 细胞测试中，SN-398 的抗肿瘤活性强于原抗肿瘤药物 SN-38 (IC50=1.562 μM)。SN-398 可用于研究 Topo I 在癌细胞中的抗增殖和抑制生长效应。

Anticanceragent 217 (35B) 是一种源自喜树碱的化合物，其对MCF-7细胞和MDA-MB-231细胞的IC50值分别为6.2 nM和7.1 nM。

Anticanceragent 219 (P139) 是喜树碱类化合物，具有抗癌活性。

Fagopyrine 作为一种光敏剂，主要用于肿瘤的研究领域。此外，它还能抑制 DNA 拓扑异构酶 I (Topo I)，显示出其潜在的生物医药价值。

Topoisomerase inhibitor3 (compound 9) 是一种拓扑异构酶 (Topoisomerase) 的高效抑制剂，具有显著的抗增殖和抗肿瘤活性。

A-1062, a resolvase-binding inhibitor, inhibits resolvase binding to the res site.

8-Chloro-ATP（8-Cl-cAMP），一种c-AMP的类似物，是一种新型的抗肿瘤化合物。

Ro 47-3359 is a topoisomerase II-targeted drugs with cytotoxic potential.

S39625, an E-ring camptothecin keto analogue, is a stable, potent, and selective topoisomerase I inhibitor without being substrates of drug efflux transporters. Nanomolar concentrations of S39625 induces intense and persistent histone gamma-H2AX. The chem

Topi MF-6 是一种DNA 拓扑异构酶 I (Top1) 抑制剂，对胃肠道癌细胞展现出卓越的细胞毒性，并可用作ADC payload。