Topoisomerase

Isoform-selective Products

Signaling Pathway

Topoisomerase Signaling Pathway

Topoisomerase Products

  • All (57)
  • Topoisomerase Inhibitors (56)
  • Topoisomerase Activator (1)
  • New Topoisomerase Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1208 Doxorubicin (DOX) HCl Doxorubicin (DOX) HCl is an antibiotic agent that inhibits human DNA topoisomerase I and topoisomerase II with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.This product may precipitate when dissolved in PBS solution. It is recommended to prepare the stock solution in pure water and dilute with either pure water or saline to obtain the working solution.
iScience, 2024, 27(1):108667
Cell, 2023, 186(14):3013-3032.e22
Cell Stem Cell, 2023, 10.1016/j.stem.2023.09.011
S1225 Etoposide Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity which enhances double-strand and single-strand cleavage of DNA and reversibly inhibits repair by topoisomerase II binding. Etoposide induces autophagy, mitophagy and apoptosis.
bioRxiv, 2024, 10.1101/2024.01.16.575847
Cancer Discov, 2023, 13(7):1696-1719
Cell Stem Cell, 2023, 10.1016/j.stem.2023.09.011
S1288 Camptothecin (CPT) Camptothecin (CPT) is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Camptothecin induces apoptosis in cancer cells via microRNA-125b-mediated mitochondrial pathways. Phase 2.
Mol Oncol, 2024, 10.1002/1878-0261.13577
Nat Commun, 2023, 14(1):4445
Nat Commun, 2023, 14(1):3034
S2217 Irinotecan HCl Trihydrate Irinotecan HCl Trihydrate is a hydrochloride trihydrate of irinotecan (Camptosar, Campto, CPT-11) which is a topoisomerase I inhibitor with IC50 of 15.8 and 5.17 μM for LoVo cells and HT-29 cells, respectively.
Int Immunopharmacol, 2023, 119:110205
iScience, 2023, 26(7):107116
Tübingen, 2023,
S4908 SN-38 SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.
NPJ Precis Oncol, 2024, 8(1):52
Cancer Discov, 2023, 13(10):2192-2211
Cancer Discov, 2023, 13(10):2192-2211
S3035 Daunorubicin HCl Daunorubicin HCl inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis.
Cell Stem Cell, 2023, 10.1016/j.stem.2023.09.011
Int J Mol Sci, 2023, 24(16)12926
Cancers (Basel), 2023, 15(12)3112
E2516 Doxorubicin Adriamycin (Doxorubicin, Hydroxydaunorubicin), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent, inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication, and induces apoptosis, also inhibits human DNA topoisomerase I with an IC50 of 0.8 μM.
Nat Commun, 2024, 15(1):1041
Cancer Lett, 2024, 586:216695
Breast Cancer Res, 2024, 26(1):35
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.
Mol Cell, 2023, 83(13):2206-2221.e11
J Transl Med, 2023, 21(1):115
Biochem Pharmacol, 2023, 214:115681
S1231 Topotecan HCl Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis.
iScience, 2024, 27(1):108667
Cell Rep, 2023, 42(8):112925
bioRxiv, 2023, 2023.01.17.524444
S2485 Mitoxantrone 2HCl 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.
Mol Metab, 2024, 80:101873
Cell Commun Signal, 2023, 21(1):167
Int J Mol Sci, 2023, 10.3390/ijms242216375
S1198 Irinotecan Irinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.
Nat Commun, 2023, 14(1):392
Cell Rep Med, 2023, 4(9):101162
Cell Rep Med, 2023, S2666-3791(23)00315-4
S1223 Epirubicin HCl Epirubicin HCl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. Epirubicin induces apoptosis.
Front Pharmacol, 2023, 14:1189245
Neoplasia, 2023, 10.1016/j.neo.2023.100949
Front Immunol, 2022, 13:1035667
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 or by insulin with IC50 of 19 μM.
Int J Nanomedicine, 2023, 18:4647-4662
Molecules, 2023, 28(4)1919
Exp Ther Med, 2023, 26(5):516
S9321 Topotecan Topotecan(NSC609699,Nogitecan,SKFS 104864A) is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.
Cell Rep Med, 2023, 4(6):101091
Braz J Med Biol Res, 2023, 55:e12206
Clin Transl Med, 2022, 12(5):e881
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.
Drug Resist Updat, 2023, 71:101005
PLoS Biol, 2023, 21(9):e3002256
PLoS Biol, 2023, 21(9):e3002256
S1787 Teniposide Teniposide (NSC 122819, VM-26) is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL).
bioRxiv, 2023, 2023.01.17.524444
Cancers (Basel), 2022, 14(19)4883
J Pers Med, 2022, 12(2)258
S2492 Novobiocin Sodium (NSC 2382) Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin) is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria.
Nat Commun, 2023, 14(1):1390
J Clin Invest, 2023, 133(11)e165934
Nucleic Acids Res, 2023, 51(18):9920-9937
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 Betulinic acid acts as a new activator of NF-κB.Phase 1/2.
Bioact Mater, 2023, 25:594-614
J Neuroinflammation, 2023, 20(1):91
Heliyon, 2023, 9(3):e14006
S1393 Pirarubicin (NSC-333054) Pirarubicin (NSC-333054,THP) 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.
Cell Death Dis, 2022, 13(5):492
Int J Nanomedicine, 2021, 16:951-976
Pharmaceuticals (Basel), 2020, 14(1)E22
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.
Int J Oncol, 2023, 62(3)42
Comput Struct Biotechnol J, 2022, 20:2442-2454
Free Radic Biol Med, 2021, 173:64-69
S2423 (S)-10-Hydroxycamptothecin (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor with potent anti-tumor activity.
Eur J Med Res, 2023, 28(1):326
Eur J Med Res, 2023, 28(1):326
Nat Commun, 2022, 13(1):2861
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.
Viruses, 2022, 15(1)105
Nat Commun, 2019, 10(1):4217
Front Oncol, 2019, 9:1406
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
Adv Sci -Weinh), 2023, 10(30):e2301136
Adv Sci (Weinh), 2023, 10(30):e2301136
Sci Adv, 2023, 9(49):eadi6681
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.
Adv Healthc Mater, 2022, e2102117
Exp Ther Med, 2021, 21(4):332
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
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.
Mol Cell, 2020, 80(6):1104-1122.e9
Kaohsiung J Med Sci, 2020, 6
Nutr Cancer, 2017, 69(7):1088-1098
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.
Cell Death Discov, 2023, 9(1):21
Cell Death Discov, 2023, 9(1):173
J Virol, 2022, 96(15):e0187421
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
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)
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, 2023, 2023.05.25.542379
Viruses, 2022, 15(1)105
S1463 Ofloxacin Ofloxacin (DL8280) is a synthetic broad-spectrum antimicrobial agent.
Molecules, 2023, 28(3)1444
S5008 Ciprofloxacin hydrochloride Ciprofloxacin (CPX, Cetraxal, Ciloxan, Cipro, Bay-09867) 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
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). Genz-644282 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
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 that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.
Anticancer Res, 2018, 38(10):5709-5716
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.
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. Rubitecan is an oral camptothecin with antitumour activity.
Chem Biol Drug Des, 2022, 100(5):699-721
S1464 Marbofloxacin Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication.
S1509 Norfloxacin Norfloxacin (MK-0366) is a broad-spectrum antibiotic. Norfloxacin (MK-0366) targets bacterial gyrase and topoisomerase IV enzymes.
S4006 Clinafloxacin Clinafloxacin (CI-960, PD127391, AM-1091) is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae.
S6747 SW-044248 SW-044248 is a non-canonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells.
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.
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.
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).
S2271 Berberine chloride Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Adv Healthc Mater, 2023, e2300591.
Transl Oncol, 2023, 35:101712
J Biomol Struct Dyn, 2022, 1-11
E2891New Dxd Dxd(Exatecan derivative for ADC) is a potent  DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM.
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-amino-CPT (9-Aminocamptothecin, 9-AC, Aminocamptothecin, 9-amino-20(S)-camptothecin) is a Topoisomerase I inhibitor with potent anticancer activities. 9-amino-CPT (9-Aminocamptothecin) is an active, water-insoluble derivative of camptothecin.
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.
S3181 Flumequine Flumequine(R-802) is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM.
E1769New Merbarone Merbarone(NSC 336628) is a catalytic inhibitor of topoisomerase II with IC50 of 120 μM, with anti-proliferative activity against human cancer cells. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage.
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.
S1208 Doxorubicin (DOX) HCl Doxorubicin (DOX) HCl is an antibiotic agent that inhibits human DNA topoisomerase I and topoisomerase II with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.This product may precipitate when dissolved in PBS solution. It is recommended to prepare the stock solution in pure water and dilute with either pure water or saline to obtain the working solution.
iScience, 2024, 27(1):108667
Cell, 2023, 186(14):3013-3032.e22
Cell Stem Cell, 2023, 10.1016/j.stem.2023.09.011
S1225 Etoposide Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity which enhances double-strand and single-strand cleavage of DNA and reversibly inhibits repair by topoisomerase II binding. Etoposide induces autophagy, mitophagy and apoptosis.
bioRxiv, 2024, 10.1101/2024.01.16.575847
Cancer Discov, 2023, 13(7):1696-1719
Cell Stem Cell, 2023, 10.1016/j.stem.2023.09.011
S1288 Camptothecin (CPT) Camptothecin (CPT) is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Camptothecin induces apoptosis in cancer cells via microRNA-125b-mediated mitochondrial pathways. Phase 2.
Mol Oncol, 2024, 10.1002/1878-0261.13577
Nat Commun, 2023, 14(1):4445
Nat Commun, 2023, 14(1):3034
S2217 Irinotecan HCl Trihydrate Irinotecan HCl Trihydrate is a hydrochloride trihydrate of irinotecan (Camptosar, Campto, CPT-11) which is a topoisomerase I inhibitor with IC50 of 15.8 and 5.17 μM for LoVo cells and HT-29 cells, respectively.
Int Immunopharmacol, 2023, 119:110205
iScience, 2023, 26(7):107116
Tübingen, 2023,
S4908 SN-38 SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.
NPJ Precis Oncol, 2024, 8(1):52
Cancer Discov, 2023, 13(10):2192-2211
Cancer Discov, 2023, 13(10):2192-2211
S3035 Daunorubicin HCl Daunorubicin HCl inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis.
Cell Stem Cell, 2023, 10.1016/j.stem.2023.09.011
Int J Mol Sci, 2023, 24(16)12926
Cancers (Basel), 2023, 15(12)3112
E2516 Doxorubicin Adriamycin (Doxorubicin, Hydroxydaunorubicin), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent, inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication, and induces apoptosis, also inhibits human DNA topoisomerase I with an IC50 of 0.8 μM.
Nat Commun, 2024, 15(1):1041
Cancer Lett, 2024, 586:216695
Breast Cancer Res, 2024, 26(1):35
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.
Mol Cell, 2023, 83(13):2206-2221.e11
J Transl Med, 2023, 21(1):115
Biochem Pharmacol, 2023, 214:115681
S1231 Topotecan HCl Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis.
iScience, 2024, 27(1):108667
Cell Rep, 2023, 42(8):112925
bioRxiv, 2023, 2023.01.17.524444
S2485 Mitoxantrone 2HCl 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.
Mol Metab, 2024, 80:101873
Cell Commun Signal, 2023, 21(1):167
Int J Mol Sci, 2023, 10.3390/ijms242216375
S1198 Irinotecan Irinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.
Nat Commun, 2023, 14(1):392
Cell Rep Med, 2023, 4(9):101162
Cell Rep Med, 2023, S2666-3791(23)00315-4
S1223 Epirubicin HCl Epirubicin HCl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. Epirubicin induces apoptosis.
Front Pharmacol, 2023, 14:1189245
Neoplasia, 2023, 10.1016/j.neo.2023.100949
Front Immunol, 2022, 13:1035667
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 or by insulin with IC50 of 19 μM.
Int J Nanomedicine, 2023, 18:4647-4662
Molecules, 2023, 28(4)1919
Exp Ther Med, 2023, 26(5):516
S9321 Topotecan Topotecan(NSC609699,Nogitecan,SKFS 104864A) is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.
Cell Rep Med, 2023, 4(6):101091
Braz J Med Biol Res, 2023, 55:e12206
Clin Transl Med, 2022, 12(5):e881
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.
Drug Resist Updat, 2023, 71:101005
PLoS Biol, 2023, 21(9):e3002256
PLoS Biol, 2023, 21(9):e3002256
S1787 Teniposide Teniposide (NSC 122819, VM-26) is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL).
bioRxiv, 2023, 2023.01.17.524444
Cancers (Basel), 2022, 14(19)4883
J Pers Med, 2022, 12(2)258
S2492 Novobiocin Sodium (NSC 2382) Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin) is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria.
Nat Commun, 2023, 14(1):1390
J Clin Invest, 2023, 133(11)e165934
Nucleic Acids Res, 2023, 51(18):9920-9937
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 Betulinic acid acts as a new activator of NF-κB.Phase 1/2.
Bioact Mater, 2023, 25:594-614
J Neuroinflammation, 2023, 20(1):91
Heliyon, 2023, 9(3):e14006
S1393 Pirarubicin (NSC-333054) Pirarubicin (NSC-333054,THP) 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.
Cell Death Dis, 2022, 13(5):492
Int J Nanomedicine, 2021, 16:951-976
Pharmaceuticals (Basel), 2020, 14(1)E22
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.
Int J Oncol, 2023, 62(3)42
Comput Struct Biotechnol J, 2022, 20:2442-2454
Free Radic Biol Med, 2021, 173:64-69
S2423 (S)-10-Hydroxycamptothecin (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor with potent anti-tumor activity.
Eur J Med Res, 2023, 28(1):326
Eur J Med Res, 2023, 28(1):326
Nat Commun, 2022, 13(1):2861
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.
Viruses, 2022, 15(1)105
Nat Commun, 2019, 10(1):4217
Front Oncol, 2019, 9:1406
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
Adv Sci -Weinh), 2023, 10(30):e2301136
Adv Sci (Weinh), 2023, 10(30):e2301136
Sci Adv, 2023, 9(49):eadi6681
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.
Adv Healthc Mater, 2022, e2102117
Exp Ther Med, 2021, 21(4):332
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
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.
Mol Cell, 2020, 80(6):1104-1122.e9
Kaohsiung J Med Sci, 2020, 6
Nutr Cancer, 2017, 69(7):1088-1098
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.
Cell Death Discov, 2023, 9(1):21
Cell Death Discov, 2023, 9(1):173
J Virol, 2022, 96(15):e0187421
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
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)
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, 2023, 2023.05.25.542379
Viruses, 2022, 15(1)105
S1463 Ofloxacin Ofloxacin (DL8280) is a synthetic broad-spectrum antimicrobial agent.
Molecules, 2023, 28(3)1444
S5008 Ciprofloxacin hydrochloride Ciprofloxacin (CPX, Cetraxal, Ciloxan, Cipro, Bay-09867) 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
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). Genz-644282 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
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
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.
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. Rubitecan is an oral camptothecin with antitumour activity.
Chem Biol Drug Des, 2022, 100(5):699-721
S1464 Marbofloxacin Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication.
S1509 Norfloxacin Norfloxacin (MK-0366) is a broad-spectrum antibiotic. Norfloxacin (MK-0366) targets bacterial gyrase and topoisomerase IV enzymes.
S4006 Clinafloxacin Clinafloxacin (CI-960, PD127391, AM-1091) is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae.
S6747 SW-044248 SW-044248 is a non-canonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells.
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.
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.
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).
S2271 Berberine chloride Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Adv Healthc Mater, 2023, e2300591.
Transl Oncol, 2023, 35:101712
J Biomol Struct Dyn, 2022, 1-11
E2891New Dxd Dxd(Exatecan derivative for ADC) is a potent  DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM.
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-amino-CPT (9-Aminocamptothecin, 9-AC, Aminocamptothecin, 9-amino-20(S)-camptothecin) is a Topoisomerase I inhibitor with potent anticancer activities. 9-amino-CPT (9-Aminocamptothecin) is an active, water-insoluble derivative of camptothecin.
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.
S3181 Flumequine Flumequine(R-802) is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM.
E1769New Merbarone Merbarone(NSC 336628) is a catalytic inhibitor of topoisomerase II with IC50 of 120 μM, with anti-proliferative activity against human cancer cells. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage.
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.
S9634 Phenoxodiol (Haginin E) Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.
Anticancer Res, 2018, 38(10):5709-5716
E2891New Dxd Dxd(Exatecan derivative for ADC) is a potent  DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM.
E1769New Merbarone Merbarone(NSC 336628) is a catalytic inhibitor of topoisomerase II with IC50 of 120 μM, with anti-proliferative activity against human cancer cells. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage.

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