Topoisomerase Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S1228	Idarubicin HCl	Idarubicin HCl (4-demethoxydaunorubicin (NSC256439, 4-DMDR) HCl) is a hydrochloride salt form of Idarubicin which is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells with IC50 of 3.3 ng/mL in a cell-free assay. Idarubicin induces mTOR-dependent cytotoxic autophagy.	Blood Cancer Discov, 2025, 10.1158/2643-3230.BCD-24-0327 Blood Cancer Discov, 2025, 6(5):464-483 Biochem Pharmacol, 2025, 237:116914
S2485	Mitoxantrone Dihydrochloride (NSC 301739)	Mitoxantrone 2HCl is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis.	Aging Cell, 2025, e70075 Biol Open, 2025, 14(9)bio062175 J Immunother Cancer, 2024, 12(11)e009805
S1223	Epirubicin HCl	Epirubicin HCl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. Epirubicin induces apoptosis.	J Exp Clin Cancer Res, 2025, 44(1):299 J Exp Clin Cancer Res, 2025, 44(1):290 Eur J Pharm Biopharm, 2025, 216:114866
S9321	Topotecan (SKF 104864A)	Topotecan(NSC609699,Nogitecan,SKFS 104864A) is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.	Ophthalmol Sci, 2026, 6(1):100963 Oncogene, 2025, 44(6):391-405 Int J Mol Sci, 2025, 26(12)5800
S5026	Irinotecan Hydrochloride	Irinotecan (CPT-11, (+)-Irinotecan) hydrochloride is an inhibitor of Topoisomerase I (Topo I) that exhibits cytotoxicity in LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.	Elife, 2025, 13RP94488 Cell Rep Med, 2024, 5(12):101838 Drug Resist Updat, 2023, 71:101005
S1787	Teniposide	Teniposide (NSC 122819, VM-26) is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL).	iScience, 2024, 27(10):110862 Environ Mol Mutagen, 2024, 10.1002/em.22604 bioRxiv, 2023, 2023.01.17.524444
S3603	Betulinic acid	Betulinic acid (ALS-357, Lupatic acid, Betulic acid), a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. It's reported that this compound acts as a new inhibitor of NF-κB.Phase 1/2.	World J Stem Cells, 2024, 16(5):575-590 J Orthop Surg Res, 2024, 19(1):188 Bioact Mater, 2023, 25:594-614
S1222	Dexrazoxane HCl	Dexrazoxane HCl is an intracellular iron chelator, which decreases the formation of superoxide radicals, used as a cardioprotective agent; also an inhibitor of topoisomerase II	Sci Adv, 2025, 11(28):eadw1720 Mol Cell, 2024, 84(21):4059-4078.e10 J Immunother Cancer, 2024, 12(11)e009805
S7261	Beta-Lapachone	Beta-Lapachone (β-Lapachone, ARQ-501) is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.	Environ Mol Mutagen, 2024, 10.1002/em.22604 Int J Oncol, 2023, 62(3)42 ProQuest , 2023, 30489399
S2423	(S)-10-Hydroxycamptothecin	(S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor with potent anti-tumor activity.	iScience, 2024, 27(10):110862 Int J Pharm, 2024, 669:125037 Eur J Med Res, 2023, 28(1):326
S1367	Amonafide	Amonafide (NSC308847, AS1413) produces protein-associated DNA-strand breaks through a topoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage. Phase 3.	iScience, 2024, 27(10):110862 Viruses, 2022, 15(1)105 Nat Commun, 2019, 10(1):4217
S1889	Mitoxantrone	Mitoxantrone is a type II topoisomerase inhibitor with IC50 of 2.0 μM, 0.42 mM for HepG2 and MCF-7/wt cells, respectively.	Int J Mol Sci, 2025, 26(12)5800 Mar Drugs, 2025, 23(10)386 Adv Healthc Mater, 2023, 12(14):e2201434
S1940	Levofloxacin	Levofloxacin (Fluoroquinolone) is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections.	Theranostics, 2025, 15(16):7990-8011 Adv Healthc Mater, 2022, e2102117 Exp Ther Med, 2021, 21(4):332
S1465	Moxifloxacin (BAY12-8039) HCl	Moxifloxacin (Avelox, Avalox,BAY12-8039 HCl) is a fourth-generation synthetic fluoroquinolone antibacterial agent.	Microorganisms, 2022, 10(7)1421 Clin Transl Sci, 2019, 12(6):687-697 Front Microbiol, 2018, 6:336
S1327	Ellagic acid	Ellagic acid (Elagostasine, Gallogen) has antiproliferative and antioxidant property.	J Ethnopharmacol, 2024, 330:118227 Food Science and Human Wellness, 2023, 2232-2241 Mol Cell, 2020, 80(6):1104-1122.e9
S7518	Voreloxin (SNS-595) hydrochloride	Voreloxin hydrochloride (SNS-595, Vosaroxin) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.	Viruses, 2022, 15(1)105 Adv Sci (Weinh), 2020, 7(21):2001018 Apoptosis, 2019, 24(11-12):849-861
S5059	Pixantrone Maleate	Pixantrone (BBR-2778) is a novel aza-anthracenedione compound with antitumor activity. It is a weak topoisomerase II inhibitor and forms stable DNA adducts through alkylation with specificity for DNA hypermethylated sites.	bioRxiv, 2025, 2025.09.08.674976 iScience, 2024, 27(10):110862 Eur J Pharmacol, 2024, 979:176835
E8164	Daunorubicin	Daunorubicin is an anthracycline antibiotic and a cell cycle–nonspecific chemotherapeutic agent that functions by inhibiting topoisomerase II and intercalating into DNA. It is primarily indicated for the treatment of acute lymphoblastic leukemia (ALL) and acute myelogenous leukemia (AML).	Blood Cancer Discov, 2025, 10.1158/2643-3230.BCD-24-0327 Blood Cancer Discov, 2025, 6(5):464-483 Br J Pharmacol, 2025, 10.1111/bph.70158
S1756	Enoxacin	Enoxacin (AT-2266, CI919, Pd107779, NSC 629661) is an oral broad-spectrum fluoroquinolone antibacterial agent by inhibiting bacterial DNA gyrase and topoisomerase IV, used to treat a wide variety of infections.	Exp Mol Med, 2025, 57(9):1978-1995 Cell Death Discov, 2023, 9(1):21 Cell Death Discov, 2023, 9(1):173
S4604	Levofloxacin hydrate	Levofloxacin (Levaquin, Tavanic, Quixin, Iquix, Cravit) is a broad-spectrum, third-generation fluoroquinolone antibiotic and optically active L-isomer of ofloxacin with antibacterial activity. It acts by inhibiting DNA gyrase (bacterial topoisomerase II).	Adv Healthc Mater, 2022, e2102117 Exp Ther Med, 2021, 21(4):332 Front Microbiol, 2020, 10:2936
S1340	Gatifloxacin	Gatifloxacin (AM-1155, CG5501, BMS-206584) is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.	Cancer Discov, 2020, CD-20-0160 Biochem Pharmacol, 2015, 95(4):227-37
S2027	Ciprofloxacin	Ciprofloxacin (Bay o 9867,Bay q 3939) is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity, with MIC90 of 0.024-6 μM.	Nanomaterials (Basel), 2021, 11(8)1984 Environ Mol Mutagen, 2019, 60(6):513-533
E4801	Cu(II)-Elesclomol	Cu(II)-Elesclomol, a Cu2+ complex of Elesclomol, is a weak inhibitor of DNA topoisomerase I. It is also highly capable of inducing cuproptosis and apoptosis. This compound induces DNA double-strand breaks in K562 cells and causes a G1 cell cycle block. It displays anticancer activity.	Eur J Med Res, 2025, 30(1):557 Leukemia, 2024, 10.1038/s41375-024-02442-0
S3898	Hydroxy Camptothecine	Hydroxy Camptothecine (10-Hydroxycamptothecin, Hydroxycamptothecine) is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones.	iScience, 2024, 27(10):110862 Life Sci, 2020, 246:117428
S2288	Rubitecan	Rubitecan (9-NC, 9-Nitro-camptothecin, Partaject Orathecin, Partaject rubitecan, RFS 2000) is a topoisomerase I inhibitor extracted from the bark and leaves of the Camptotheca acuminata tree, which is native to China. This compound is an oral camptothecin with antitumour activity.	iScience, 2024, 27(10):110862 Chem Biol Drug Des, 2022, 100(5):699-721
S1463	Ofloxacin	Ofloxacin (DL8280) is a synthetic broad-spectrum antimicrobial agent.	Molecules, 2023, 28(3)1444
S1509	Norfloxacin	Norfloxacin (MK-0366) is a broad-spectrum antibiotic. This compound targets bacterial gyrase and topoisomerase IV enzymes.	J Chromatogr A, 2024, 1734:465286
S5008	Ciprofloxacin (CPX) hydrochloride	Ciprofloxacin (CPX) hydrochloride, a fluorinated quinolone, is a β-diketone antibiotic with a broad spectrum antibacterial activity. Ciprofloxacin is an inhibitor of bacterial DNA gyrase (a subclass of Type II topoisomerases).	Nanomaterials (Basel), 2021, 11(8)1984
E7068	Novobiocin	Novobiocin (Albamycin, Cathomycin) is a potent, orally active antibiotic and an inhibitor of DNA gyrase andtopoisomerase II, and also an antagonist of heat shock protein 90 (Hsp90). It shows potential for treating β-lactam-resistant pneumococcal infections and sensitizing brain tumors to DNA cross-linking anticancer agents.	Cancer Sci, 2025, 10.1111/cas.70081
S0093	Genz-644282	Genz-644282 is a non-camptothecin topoisomerase I (Topo I) inhibitor that demonstrates potent cytotoxic activity with a median IC50 of 1.2 nM (range 0.2 nM-21.9 nM). This compound can be used in cancer research.The solubility of this product is not good, please choose carefully for cell experiments!	Commun Biol, 2022, 5(1):982
E4925	Amsacrine	Amsacrine(m-AMSA; acridinyl anisidide) is an inhibitor of topoisomerase II. This compound acts as an antineoplastic agent which intercalates into the DNA of tumor cells, it is also used in the treatment of acute myelogenous leukemia.	Nucleic Acids Res, 2024, 52(18):11301-11316
S6631	Belotecan (CKD-602) hydrochloride	Belotecan (CKD-602) is a potent DNA topoisomerase I inhibitor that exerts a clinical anticancer effect on various types of tumor.	iScience, 2024, 27(10):110862
E1769	Merbarone	Merbarone (NSC 336628) is a catalytic inhibitor of topoisomerase II with IC50 of 120 μM, with anti-proliferative activity against human cancer cells. This compound acts primarily by blocking topoisomerase II-mediated DNA cleavage.	Cancer Sci, 2025, 10.1111/cas.70081
S1464	Marbofloxacin	Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication.
S4006	Clinafloxacin	Clinafloxacin (CI-960, PD127391, AM-1091) is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae.
E8269^New	Eleutherin	Eleutherin ((+)-Eleutherin) is a pyranonaphthoquinones that is isolated from the bulb of Eleutherine americana and a potent catalytic inhibitor of Topoisomerase II. This compound exhibits potent anti-cancer activity and protects human umbilical vein endothelial cells (HUVECs) from injury in vitro.
E8306^New	ABBV-969 Payload	ABBV-969 Payload is an agent-linker conjugate with a potent inhibitor of topoisomerase I and a linker designed for use in the antibody-drug conjugate (ADC) ABBV-969. It can be used in non-small cell lung cancer research.
S6747	SW-044248	SW-044248 is a non-canonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells.
E4708^New	Etoposide phosphate	Etoposide phosphate a phosphate ester proagent of etoposide, is a selective inhibitor of topoisomerase II and a potent anti-cancer chemotherapy agent. This compound also induces cell cycle arrest, apoptosis, and autophagy.
S4119	Pefloxacin Mesylate Dihydrate	Pefloxacin Mesylate Dihydrate (1589 RB,Pefloxacinium mesylate dihydrate) is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication.
S5627	Amsacrine hydrochloride	Amsacrine hydrochloride (m-AMSA, acridinyl anisidide) is the hydrochloride salt form of amsacrine, which is an inhibitor of topoisomerase II with antineoplastic activity.
E1592	Gepotidacin	Gepotidacin (GSK2140944) is a triazaacenaphthylene that inhibits bacterial type II topoisomerases. It has the potential to treat conventional and biothreat pathogens, including Gram-positive bacteria and methicillin-resistant Staphylococcus aureus (MRSA).
S5964	Gatifloxacin hydrochloride	Gatifloxacin (AM-1155, CG5501, BMS-206584, PD135432) hydrochloride is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases with IC50 of 13.8 μg/ml and 0.109 μg/ml for S. aureus topoisomerase IV and E. coli DNA gyrase, respectively.
S2064	Balofloxacin	Balofloxacin (Q-35,Q-roxin) is a quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase.
E1905	Nalidixic acid sodium salt	Nalidixic acid sodium salt is an inhibitor of bacterial DNA gyrase and topoisomerase IV, essential enzymes for DNA supercoiling during replication, making it an effective quinolone antibiotic against both gram-positive and gram-negative bacteria.
E6461^New	Cholesteryl hemisuccinate	Cholesteryl hemisuccinate is a cholesterol derivative and a potent inhibior of DNA polymerase and DNA topoisomerase with an IC50 of 2.9 μM, 6.3 μM, 25 μM for Rat DNA polymerase β, Human DNA polymerase λ and Human DNA topoisomerase I respectively. It exhibits anticancer effect due to its ability to inhibit DNA replication, repair and cell division and can be used in cancer cell growth research.
E4811	Levofloxacin hydrochloride	Levofloxacin hydrochloride ((-)-Ofloxacin hydrochloride), a synthetic fluoroquinolone antibiotic, is an inhibitor of DNA gyrase and Topoisomerase IV. It exhibits bactericidal effects by preventing bacterial DNA replication.
E2891	Dxd (Exatecan derivative for ADC)	Dxd(Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM.
E6034	Trovafloxacin	Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1.
E7100	Ellipticine	Ellipticine (NSC 71795) is a potent antitumor alkaloid that inhibits the activity of DNA topoisomerase II. It acts by intercalating into DNA, causing DNA damage and inducing cytotoxicity. It also can disrupt mitochondrial oxidative phosphorylation and exhibits potential antineoplastic effects.
E5775	Exatecan	Exatecan (DX-8951), is a water-soluble derivative of camptothecin. It acts as an inhibitor of DNA topoisomerase I with an IC50 value of 1.906 μM. It demonstrates potent antitumor effects and triggers apoptotic cell death after treatment in human pancreatic cancer cells.
S5111	7-Ethylcamptothecin	7-Ethyl Camptothecin is an anti-cancer chemical that exhibits a strong activity against various murine tumors through Topo I (topoisomerase) inhibition.
S2653	9-amino-CPT (9-Aminocamptothecin)	9-Aminocamptothecin (9-amino-CPT, 9-AC, Aminocamptothecin, 9-amino-20(S)-camptothecin) is a Topoisomerase I inhibitor with potent anticancer activities. It is an active, water-insoluble derivative of camptothecin.
S3181	Flumequine	Flumequine (R-802) is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM.
S8999	Exatecan Mesylate	Exatecan Mesylate (DX-8951f) is a water-soluble and non-pro-drug analog of camptothecin and shows significant topoisomerase I inhibition with IC50 of 0.975 μg/ml.
S1342	Genistein	Genistein, a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM.	J Immunother Cancer, 2025, 13(6)e011442 Cell Rep, 2025, 44(6):115849 Cell Death Dis, 2024, 15(11):855
S1393	Pirarubicin	Pirarubicin is an anthracycline antibiotic, and also a DNA/RNA synthesis inhibitor by intercalating into DNA and interacts with topoisomerase II, used as an antineoplastic agent.	PLoS Biol, 2024, 22(7):e3002547 iScience, 2024, 27(10):110862 Biomed Pharmacother, 2023, 163:114751
S2271	Berberine chloride	Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. This compound activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. It decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. This chemical induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. It is a dual topoisomerase I and II inhibitor. It is also a potential autophagy modulator.	J Cardiovasc Dev Dis, 2025, 12(7)278 Adv Healthc Mater, 2023, e2300591. Transl Oncol, 2023, 35:101712
S5686	Tryptanthrin	Tryptanthrin is a natural alkaloidal compound having basic indoloquinazoline moiety. It has broad spectrum of biological activities including anticancer activity, anti-inflammatory, antiprotozoal, antiallergic, antioxidant, and antimicrobial.	J Org Chem, 2025, 90(29):10434-10441 Redox Biol, 2024, 76:103323 BMC Complement Med Ther, 2024, 24(1):28
S2328	Nalidixic acid	Nalidixic acid (NSC-82174) is a synthetic 1,8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum. It is an inhibitor of the A subunit of bacterial DNA gyrase.	Hum Mol Genet, 2020, ddaa244 Int J Mol Sci, 2018, 19(6)
S8942	Suramin sodium salt	Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatase (PTPases) inhibitor, also is the potent inhibitor of sirtuins, purified topoisomerase II and SARS-CoV-2 RNA-dependent RNA polymerase (RdRp).	Biol Pharm Bull, 2025, 48(5):657-671 J Biol Chem, 2024, S0021-9258(24)00128-5
S6790	Ellipticine hydrochloride	Ellipticine Hydrochloride (NSC 71795, PZE) is a potent inhibitor of DNA topoisomerase II and forms covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases. Ellipticine Hydrochloride is a natural product isolated from the Australian evergreen tree of the Apocynaceae family with antineoplastic activity.	Viruses, 2022, 15(1)105
S9634	Phenoxodiol (Haginin E)	Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity. It activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. This compound also inhibits DNA topoisomerase II.	Anticancer Res, 2018, 38(10):5709-5716
S2469	Fleroxacin	Fleroxacin (Ro 23-6240,AM-833,Quinodis, Megalocin) is a new broad-spectrum fluoroquinolone.
S1884	Sparfloxacin	Sparfloxacin (AT-4140, CI-978, PD 131501,Zagam) is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity.
E0706	Gemifloxacin mesylate	Gemifloxacin mesylate (SB265805 mesylate; LB20304 mesylate) is a novel fluoronaphthyridone with a broad spectrum of antimicrobial activity and enhances activity against gram-positive aerobes.
S5209	Enoxacin Sesquihydrate	Enoxacin sesquihydrate (Enoxacin hydrate) is a broad-spectrum 6-fluoronaphthyridinone antibacterial agent.
S9795	Deruxtecan	Deruxtecan is an ADC drug-linker conjugate composed of the cleavable glycine–glycine–phenylalanine–glycine tetrapeptide-based linker, a self-immolative amino methylene spacer, and a novel topoisomerase 1 inhibitor payload that is a derivative of exatecan (DX-8951).