Topoisomerase

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Topoisomerase Products

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Catalog No. Product Name Information Product Use Citations Product Validations
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.
S1198 Irinotecan (CPT-11) Irinotecan (CPT-11, (+)-Irinotecan) is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.
Cancers (Basel), 2022, 14(5)1230
Cancer Cell, 2021, 39(4):566-579.e7
J Cachexia Sarcopenia Muscle, 2021, 10.1002/jcsm.12703
S1208 Doxorubicin (Adriamycin) HCl Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. 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.
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
EMBO Mol Med, 2022, 14(2):e14903
EMBO J, 2022, 10.15252/embj.2021108599
S1222 Dexrazoxane HCl (ICRF-187) Dexrazoxane HCl (ICRF-187, ADR-529) is an intracellular iron chelator, which decreases the formation of superoxide radicals, used as a cardioprotective agent; also an inhibitor of topoisomerase II
PLoS Genet, 2019, 15(2):e1007925
J Virol, 2019, 93(11)
EMBO Rep, 2017, 18(8):1412-1428
S1223 Epirubicin (IMI 28) HCl Epirubicin HCl (IMI 28, NSC 256942, 4'-epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. Epirubicin induces apoptosis.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancer Cell, 2021, S1535-6108(20)30609-7
Cell Rep, 2021, 34(10):108814
S1225 Etoposide (VP-16) Etoposide (VP-16, VP-16213) is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity. Etoposide induces autophagy, mitophagy and apoptosis.
Mol Cell, 2022, S1097-2765(22)00085-5
Dev Cell, 2022, 57(5):638-653.e5
Cancers (Basel), 2022, 14(6)1537
S1228 Idarubicin HCl Idarubicin HCl (4-demethoxydaunorubicin, NSC256439, 4-DMDR) 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.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancers (Basel), 2021, 13(14)3586
Biomolecules, 2021, 11(8)1128
S1231 Topotecan (NSC609699) HCl Topotecan HCl (NSC609699, Nogitecan, SKFS 104864A) 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.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancer Cell, 2021, S1535-6108(21)00659-0
Cancer Res, 2021, canres.1540.2020
S1288 Camptothecin (NSC-100880) Camptothecin (NSC-100880, CPT, Campathecin, (S)-(+)-Camptothecin) 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.
Sci Adv, 2022, 8(3):eabj8357
Cell Rep, 2022, 38(12):110536
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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
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
S1342 Genistein (NPI 031L) Genistein (NPI 031L), 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.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Adv Sci (Weinh), 2021, e2103360
Nat Chem Biol, 2021, 10.1038/s41589-021-00772-z
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.
Nat Commun, 2019, 10(1):4217
Front Oncol, 2019, 9:1406
Theranostics, 2015, 5(5):477-88
S1393 Pirarubicin (NSC-333054) Pirarubicin (NSC-333054) 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.
Int J Nanomedicine, 2021, 16:951-976
Pharmaceuticals (Basel), 2020, 14(1)E22
Cancer Cell, 2019, 36(2):179-193
S1463 Ofloxacin Ofloxacin (DL8280) is a synthetic broad-spectrum antimicrobial agent.
S1464 Marbofloxacin Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication.
S1465 Moxifloxacin (BAY12-8039) HCl Moxifloxacin (BAY12-8039) is a fourth-generation synthetic fluoroquinolone antibacterial agent.
Clin Transl Sci, 2019, 12(6):687-697
Front Microbiol, 2018, 6:336
J Pharmacol Toxicol Methods, 2017, 90:39-47
S1509 Norfloxacin Norfloxacin (MK-0366) is a broad-spectrum antibiotic. Norfloxacin (MK-0366) targets bacterial gyrase and topoisomerase IV enzymes.
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.
J Virol, 2020, 17;94(3) pii: e01233-19
S1787 Teniposide Teniposide (NSC 122819, VM-26) is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL).
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancer Cell, 2021, S1535-6108(21)00659-0
Nat Commun, 2021, 12(1):6813
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
S2027 Ciprofloxacin Ciprofloxacin (Bay o 9867) is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity, with MIC90 of 0.024-6 μM.
Environ Mol Mutagen, 2019, 60(6):513-533
S2064 Balofloxacin Balofloxacin (Q-35) is a quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase.
S2217 Irinotecan (CPT-11) HCl Trihydrate Irinotecan (CPT-11) prevents DNA from unwinding by inhibition of topoisomerase 1.
Cancers (Basel), 2022, 14(5)1230
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Adv Sci (Weinh), 2021, e2103360
S2271 Berberine chloride (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18) 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.
Front Pharmacol, 2021, 12:632201
Molecules, 2021, 26(5)1210
Biology (Basel), 2021, 10(3)250
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.
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)
S2423 (S)-10-Hydroxycamptothecin (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor with potent anti-tumor activity.
ACS Appl Mater Interfaces, 2021, 13(47):56519-56529
Carcinogenesis, 2021, bgab002
Vet Microbiol, 2021, 265:109313
S2485 Mitoxantrone (NSC-301739) 2HCl Mitoxantrone 2HCl (NSC-301739) 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.
J Cell Biochem, 2022, 10.1002/jcb.30213
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancers (Basel), 2021, 13(8)1954
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.
Mol Cancer Ther, 2021, 10.1158/1535-7163.MCT-21-0215
Nat Cancer, 2021, 2(6):598-610
Mol Syst Biol, 2018, 14(3):e7858
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.
S3035 Daunorubicin (RP 13057) HCl Daunorubicin HCl (Daunomycin, RP 13057, Rubidomycin) 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.
Nat Cell Biol, 2022, 10.1038/s41556-021-00814-7
Cell Rep, 2022, 39(1):110643
J Cell Biochem, 2022, 10.1002/jcb.30213
S3181 Flumequine Flumequine is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM.
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. Betulinic acid acts as a new activator of NF-kB.Phase 1/2.
Oxid Med Cell Longev, 2021, 2021:5519587
J Cardiovasc Pharmacol, 2021, 78(2):235-246
Acta Biochim Biophys Sin (Shanghai), 2021, gmab111
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
S4006 Clinafloxacin Clinafloxacin (CI-960, PD127391, AM-1091) is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae.
S4119 Pefloxacin Mesylate Dihydrate Pefloxacin Mesylate Dihydrate (1589 RB) is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication.
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
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.
Biomedicines, 2022, 10(3)638
Cell, 2021, 184(25):6119-6137.e26
Cancer Cell, 2021, S1535-6108(21)00659-0
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).
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.
Cancers (Basel), 2022, 14(5)1230
Biomedicines, 2022, 10(2)438
Biomaterials, 2021, 280:121276
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.
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.
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.
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.
S6747 SW-044248 SW-044248 is a non-canonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells.
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.
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.
Free Radic Biol Med, 2021, 173:64-69
Mutagenesis, 2021, geab014
Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0220-1
S7518 Voreloxin (SNS-595) hydrochloride Voreloxin hydrochloride (SNS-595, Vosaroxin) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.
Adv Sci (Weinh), 2020, 7(21):2001018
Apoptosis, 2019, 24(11-12):849-861
Target Oncol, 2019, 14(3):351-364
S8999New 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.
S9321 Topotecan Topotecan is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.
Nat Commun, 2021, 12(1):5404
J Exp Clin Cancer Res, 2021, 40(1):276
Cancers (Basel), 2021, 13(14)3586
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
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.
S1198 Irinotecan (CPT-11) Irinotecan (CPT-11, (+)-Irinotecan) is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.
Cancers (Basel), 2022, 14(5)1230
Cancer Cell, 2021, 39(4):566-579.e7
J Cachexia Sarcopenia Muscle, 2021, 10.1002/jcsm.12703
S1208 Doxorubicin (Adriamycin) HCl Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. 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.
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
EMBO Mol Med, 2022, 14(2):e14903
EMBO J, 2022, 10.15252/embj.2021108599
S1222 Dexrazoxane HCl (ICRF-187) Dexrazoxane HCl (ICRF-187, ADR-529) is an intracellular iron chelator, which decreases the formation of superoxide radicals, used as a cardioprotective agent; also an inhibitor of topoisomerase II
PLoS Genet, 2019, 15(2):e1007925
J Virol, 2019, 93(11)
EMBO Rep, 2017, 18(8):1412-1428
S1223 Epirubicin (IMI 28) HCl Epirubicin HCl (IMI 28, NSC 256942, 4'-epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. Epirubicin induces apoptosis.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancer Cell, 2021, S1535-6108(20)30609-7
Cell Rep, 2021, 34(10):108814
S1225 Etoposide (VP-16) Etoposide (VP-16, VP-16213) is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity. Etoposide induces autophagy, mitophagy and apoptosis.
Mol Cell, 2022, S1097-2765(22)00085-5
Dev Cell, 2022, 57(5):638-653.e5
Cancers (Basel), 2022, 14(6)1537
S1228 Idarubicin HCl Idarubicin HCl (4-demethoxydaunorubicin, NSC256439, 4-DMDR) 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.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancers (Basel), 2021, 13(14)3586
Biomolecules, 2021, 11(8)1128
S1231 Topotecan (NSC609699) HCl Topotecan HCl (NSC609699, Nogitecan, SKFS 104864A) 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.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancer Cell, 2021, S1535-6108(21)00659-0
Cancer Res, 2021, canres.1540.2020
S1288 Camptothecin (NSC-100880) Camptothecin (NSC-100880, CPT, Campathecin, (S)-(+)-Camptothecin) 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.
Sci Adv, 2022, 8(3):eabj8357
Cell Rep, 2022, 38(12):110536
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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
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
S1342 Genistein (NPI 031L) Genistein (NPI 031L), 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.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Adv Sci (Weinh), 2021, e2103360
Nat Chem Biol, 2021, 10.1038/s41589-021-00772-z
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.
Nat Commun, 2019, 10(1):4217
Front Oncol, 2019, 9:1406
Theranostics, 2015, 5(5):477-88
S1393 Pirarubicin (NSC-333054) Pirarubicin (NSC-333054) 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.
Int J Nanomedicine, 2021, 16:951-976
Pharmaceuticals (Basel), 2020, 14(1)E22
Cancer Cell, 2019, 36(2):179-193
S1463 Ofloxacin Ofloxacin (DL8280) is a synthetic broad-spectrum antimicrobial agent.
S1464 Marbofloxacin Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication.
S1465 Moxifloxacin (BAY12-8039) HCl Moxifloxacin (BAY12-8039) is a fourth-generation synthetic fluoroquinolone antibacterial agent.
Clin Transl Sci, 2019, 12(6):687-697
Front Microbiol, 2018, 6:336
J Pharmacol Toxicol Methods, 2017, 90:39-47
S1509 Norfloxacin Norfloxacin (MK-0366) is a broad-spectrum antibiotic. Norfloxacin (MK-0366) targets bacterial gyrase and topoisomerase IV enzymes.
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.
J Virol, 2020, 17;94(3) pii: e01233-19
S1787 Teniposide Teniposide (NSC 122819, VM-26) is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL).
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancer Cell, 2021, S1535-6108(21)00659-0
Nat Commun, 2021, 12(1):6813
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
S2027 Ciprofloxacin Ciprofloxacin (Bay o 9867) is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity, with MIC90 of 0.024-6 μM.
Environ Mol Mutagen, 2019, 60(6):513-533
S2064 Balofloxacin Balofloxacin (Q-35) is a quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase.
S2217 Irinotecan (CPT-11) HCl Trihydrate Irinotecan (CPT-11) prevents DNA from unwinding by inhibition of topoisomerase 1.
Cancers (Basel), 2022, 14(5)1230
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Adv Sci (Weinh), 2021, e2103360
S2271 Berberine chloride (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18) 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.
Front Pharmacol, 2021, 12:632201
Molecules, 2021, 26(5)1210
Biology (Basel), 2021, 10(3)250
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.
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)
S2423 (S)-10-Hydroxycamptothecin (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor with potent anti-tumor activity.
ACS Appl Mater Interfaces, 2021, 13(47):56519-56529
Carcinogenesis, 2021, bgab002
Vet Microbiol, 2021, 265:109313
S2485 Mitoxantrone (NSC-301739) 2HCl Mitoxantrone 2HCl (NSC-301739) 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.
J Cell Biochem, 2022, 10.1002/jcb.30213
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancers (Basel), 2021, 13(8)1954
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.
Mol Cancer Ther, 2021, 10.1158/1535-7163.MCT-21-0215
Nat Cancer, 2021, 2(6):598-610
Mol Syst Biol, 2018, 14(3):e7858
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.
S3035 Daunorubicin (RP 13057) HCl Daunorubicin HCl (Daunomycin, RP 13057, Rubidomycin) 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.
Nat Cell Biol, 2022, 10.1038/s41556-021-00814-7
Cell Rep, 2022, 39(1):110643
J Cell Biochem, 2022, 10.1002/jcb.30213
S3181 Flumequine Flumequine is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM.
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. Betulinic acid acts as a new activator of NF-kB.Phase 1/2.
Oxid Med Cell Longev, 2021, 2021:5519587
J Cardiovasc Pharmacol, 2021, 78(2):235-246
Acta Biochim Biophys Sin (Shanghai), 2021, gmab111
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
S4006 Clinafloxacin Clinafloxacin (CI-960, PD127391, AM-1091) is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae.
S4119 Pefloxacin Mesylate Dihydrate Pefloxacin Mesylate Dihydrate (1589 RB) is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication.
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
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.
Biomedicines, 2022, 10(3)638
Cell, 2021, 184(25):6119-6137.e26
Cancer Cell, 2021, S1535-6108(21)00659-0
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).
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.
Cancers (Basel), 2022, 14(5)1230
Biomedicines, 2022, 10(2)438
Biomaterials, 2021, 280:121276
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.
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.
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.
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.
S6747 SW-044248 SW-044248 is a non-canonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells.
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.
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.
Free Radic Biol Med, 2021, 173:64-69
Mutagenesis, 2021, geab014
Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0220-1
S7518 Voreloxin (SNS-595) hydrochloride Voreloxin hydrochloride (SNS-595, Vosaroxin) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.
Adv Sci (Weinh), 2020, 7(21):2001018
Apoptosis, 2019, 24(11-12):849-861
Target Oncol, 2019, 14(3):351-364
S8999New 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.
S9321 Topotecan Topotecan is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.
Nat Commun, 2021, 12(1):5404
J Exp Clin Cancer Res, 2021, 40(1):276
Cancers (Basel), 2021, 13(14)3586
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
S8999New 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.