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Topoisomerase

Topoisomerase

Inhibitory Selectivity

Catalog No.	Inhibitor Name	Topoisomerase	Topo I	Topo II	Other
A10174	Camptothecin		**
A10939	Topotecan HCl		****
A10465	Idarubicin HCl			***	Multicellular spheroids
A10194	Daunorubicin HCl	***
A11999	Betulinic acid		**		HIV-1,Aminopeptidase N
A11861	Flumequine			*
A14403	Doxorubicin
A10373	Etoposide
A10478	Irinotecan
A10345	Epirubicin HCl
A10596	Mitoxantrone HCl
A10609	Moxifloxacin HCl
A10479	Irinotecan HCl Trihydrate
A12011	SN-38
A10071	Amonafide
A10907	Teniposide
A10419	Gatifloxacin
A10426	Genistein				EGFR
A10595	Mitoxantrone
A10735	Pirarubicin
A10041	Adriamycin
A10557	Marbofloxacin
A10666	Ofloxacin
A10740	Podophyllotoxin
A12663	Amrubicin
A13059	Beta-Lapachone				IDO1

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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Karenitecin

Catalog No. A21156
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topoisomerase I inhibitor

Karenitecin (Cositecan) is a topoisomerase I inhibitor, with potent anti-cancer activity. 了解更多

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Edotecarin

Catalog No. A21233
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Topoisomerase I inhibitor

Edotecarin is a potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage, with IC50 of 50 nM. 了解更多

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Exatecan Mesylate

Catalog No. A21515
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DNA topoisomerase I inhibitor

Exatecan Mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research. 了解更多

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Dxd

Catalog No. A21517
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DNA topoisomerase I inhibitor

Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a). 了解更多

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Daun02

Catalog No. A21818
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prodrug of the topoisomerase inhibitor Daunorubicin

Daun02 is a prodrug of the topoisomerase inhibitor Daunorubicin. 了解更多

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Daunorubicin

Catalog No. A21903
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topoisomerase II inhibitor

Daunorubicin (Daunomycin; RP 13057; Rubidomycin) is a topoisomerase II inhibitor with potent antineoplastic activities. 了解更多

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TAS-103

Catalog No. A21954
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DNA topoisomerase I/II inhibitor

TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research. 了解更多

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Moxifloxacin HCl

Catalog No. A10609
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Topoisomerase 抑制剂

Moxifloxacin HCl是一种喹诺酮/氟喹诺酮类抗菌剂。了解更多

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- Hiroshi Arakawa, .et al. Possible interaction of quinolone antibiotics with peptide transporter 1 in oral absorption of peptide-mimetic drugs, Biopharm Drug Dispos, 2016, Jan;37(1):39-45 PMID: 26590007
- Arisa Higa, .et al. Differing responses of human stem cell-derived cardiomyocytes to arrhythmogenic drugs, determined using impedance measurements, Fundam. Toxicol. Sci, 2016, 3(2): 47-53
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(-)-Epigallocatechin gallate

Catalog No. A10005
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Antioxidant, antiangiogenic, antitumor agent

(-)-Epigallocatechin gallate是一种从绿茶中分离出来的强效抗氧化剂多酚类黄酮。了解更多

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- Wafa Dridi, .et al. Influence of polysaccharide concentration on polyphenol-polysaccharide interactions, Carbohydr Polym, 2021, 274:118670 PMID: 34702486
- A S D'Costa, .et al. Inhibition of starch digestion by flavonoids: Role of flavonoid-amylase binding kinetics, Food Chem, 2020, Oct 1;341(Pt 2):128256 PMID: 33035827
- Fenteany G, .et al. Multilevel structure-activity profiling reveals multiple green tea compound families that each modulate ubiquitin-activating enzyme and ubiquitination by a distinct mechanism, Sci Rep, 2019, Sep 5;9(1):12801 PMID: 31488855
- LiliSun, .et al. Comparative Effect of Black, Green, Oolong and White Tea Intake on Body Weight Gain and Bile Acid Metabolism, Nutrition, 2019, pii:S0899-9007(18)31140-7
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9-amino-CPT

Catalog No. A12540
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Topoisomerase I inhibitor

9-Aminocamptothecin is a topoisomerase I inhibitor with potent anticancer activity. 了解更多

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Epirubicin

Catalog No. A12409
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Topoisomerase 抑制剂

Epirubicin是一种细胞可渗透的抗肿瘤抗生素。阿霉素的立体异构体，其心脏毒性降低。表柔比星的抗肿瘤作用是通过靶向和抑制Topo II（拓扑异构酶II）来介导的。了解更多

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- Xiu-wu Pan, .et al. Icaritin acts synergistically with epirubicin to suppress bladder cancer growth through inhibition of autophagy, Oncol Rep, 2016, Jan;35(1):334-42 PMID: 26496799
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MAC glucuronide phenol-linked SN-38

Catalog No. A18403
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DNA topoisomerase I inhibitor

MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) drug linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively. 了解更多

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CL2A-SN-38

Catalog No. A18392
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DNA Topoisomerase I inhibitor

CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. 了解更多

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Amonafide (AS1413)

Catalog No. A10071
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Topoisomerase 抑制剂

Amonafide (AS1413)是一种DNA插入剂和拓扑异构酶II抑制剂，是治疗肿瘤疾病的抗肿瘤药物之一。了解更多

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- Veronica Rendo, .et al. Exploiting loss of heterozygosity for allele-selective colorectal cancer chemotherapy, Nat Commun, 2020, 11: 1308 PMID: 32161261
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GENZ-644282

Catalog No. A13206
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topoisomerase 1 抑制剂

GENZ-644282是拓扑异构酶I的非喜树碱抑制剂，具有潜在的抗肿瘤活性。了解更多

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Beta-Lapachone

Catalog No. A13059
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DNA topoisomerase II 抑制剂

Beta-Lapachone是一种选择性的DNA拓扑异构酶I抑制剂，对DNA拓扑异构酶II或连接酶没有抑制活性。了解更多

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- Xiaoling Li, .et al. Nanozyme-Augmented Tumor Catalytic Therapy by Self-Supplied H2O2 Generation, ACS Appl. Bio Mater, 2020, 3, 3, 1769-1778
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SN 38

Catalog No. A12011
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DNA topoisomerase 抑制剂

SN 38是依立替康(喜树碱的类似物-拓扑异构酶I抑制剂)的活性代谢物。了解更多

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- Chen JC, .et al. In Vitro and In Silico Mechanistic Insights into miR-21-5p-Mediated Topoisomerase Drug Resistance in Human Colorectal Cancer Cells, Biomolecules, 2019, Sep 9;9(9) PMID: 31505885
- Alibolandi M, .et al. Tetrac-decorated chitosan-coated PLGA nanoparticles as a new platform for targeted delivery of SN38, Artif Cells Nanomed Biotechnol, 2018, May 27:1-12 PMID: 29806500
- Bar-Zeev M, .et al. β-Casein micelles for oral delivery of SN-38 and elacridar to overcome BCRP-mediated multidrug resistance in gastric cancer, Eur J Pharm Biopharm, 2018, Dec;133:240-249 PMID: 30367935
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Etoposide (VP-16)

Catalog No. A10373
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Topoisomerase II 抑制剂

Etoposide (VP-16)是通过抑制topoisomerase II活性而抑制DNA合成。了解更多

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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Chen JC, .et al. In Vitro and In Silico Mechanistic Insights into miR-21-5p-Mediated Topoisomerase Drug Resistance in Human Colorectal Cancer Cells, Biomolecules, 2019, Sep 9;9(9) PMID: 31505885
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Calhelha RC, .et al. Mathematical models of cytotoxic effects in endpoint tumor cell line assays: critical assessment of the application of a single parametric value as a standard criterion to quantify the dose-response effects and new unexplored proposal formats, Analyst, 2017, Oct 23;142(21):4124-4141 PMID: 28991301
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Genistin (Genistoside)

Catalog No. A10426
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Genistin (Genistoside)是一种异黄酮，存在于许多饮食植物中，如大豆和葛根。显示出刺激体内雌激素依赖性乳腺癌细胞生长。了解更多

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- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Idarubicin HCl

Catalog No. A10465
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Topoisomerase 抑制剂

Idarubicin HCl是蒽环类抗生素，是一种比柔红霉素具有更高DNA结合能力和更大细胞毒性的抗白血病药物。了解更多

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- Wei Y, .et al. SUMO-Targeted DNA Translocase Rrp2 Protects the Genome from Top2-Induced DNA Damage, Mol Cell, 2017, Jun 1;66(5):581-596.e6 PMID: 28552615
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ABT 492 meglumine (Delafloxacin meglumine)

Catalog No. A15064
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ABT 492 meglumine (Delafloxacin meglumine)对喹诺酮敏感和耐药的革兰氏阳性生物更有力，对环丙沙星家族肠杆菌科的某些成员具有类似于环丙沙星的活性，对喹诺酮敏感，非发酵性，革兰氏阴性生物具有类似的活性。了解更多

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- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Irinotecan

Catalog No. A10478
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Topoisomerase I 抑制剂

Irinotecan通过抑制拓扑异构酶防止DNA解链。了解更多

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- Gils Jose, .et al. Co-Delivery of CPT-11 and Panobinostat with Anti-GD2 Antibody Conjugated Immunoliposomes for Targeted Combination Chemotherapy, Cancers (Basel), 2020, Oct 31;12(11):E3211 PMID: 33142721
- T Kannathasan, .et al. Chemoresistance-Associated Silencing of miR-4454 Promotes Colorectal Cancer Aggression through the GNL3L and NF-κB Pathway, Cancers (Basel), 2020, May; 12(5): 1231 PMID: 32422901
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NK314

Catalog No. A13993
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Topoisomerase II 抑制剂

NK314是一种新型的合成苯并[c]菲啶生物碱，具有很强的抗肿瘤活性。它抑制拓扑异构酶II活性并稳定拓扑异构酶II-DNA可裂解的复合物。了解更多

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- Kopa P, .et al. Inhibition of DNA-PK potentiates the synergistic effect of NK314 and etoposide combination on human glioblastoma cells, Mol Biol Rep, 2019, Oct 3 PMID: 31583565
- Macieja A, .et al. Comparison of the effect of three different topoisomerase II inhibitors combined with cisplatin in human glioblastoma cells sensitized with double strand break repair inhibitors, Mol Biol Rep, 2019, Apr 24 PMID: 31020489
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Ellipticine

Catalog No. A13780
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DNA topoisomerase II 抑制剂

Ellipticine是DNA嵌入剂和DNA拓扑异构酶II抑制剂。了解更多

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- Calhelha RC, .et al. Mathematical models of cytotoxic effects in endpoint tumor cell line assays: critical assessment of the application of a single parametric value as a standard criterion to quantify the dose-response effects and new unexplored proposal formats, Analyst, 2017, Oct 23;142(21):4124-4141 PMID: 28991301
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Doxorubicin

Catalog No. A14403
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Topoisomerase II 抑制剂

Doxorubicin是一种抑制DNA拓扑异构酶II并诱导DNA损伤和凋亡的抗生素。了解更多

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- J Priyanga, .et al. A novel indenone derivative selectively induces senescence in MDA-MB-231 (breast adenocarcinoma) cells, Chem Biol Interact, 2020, Nov 1;331:109250 PMID: 32956706
- Abdelrehim A, .et al. The use of tail-anchored protein chimeras to enhance liposomal cargo delivery, PLoS One, 2019, Feb 22;14(2):e0212701 PMID: 30794671
- J Wei, .et al. Profiling the surface proteome identifies actionable biology for TSC1 mutant cells beyond mTORC1 signaling, bioRxiv, 2018, 2018