Topoisomerase

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S1208

Doxorubicin (Adriamycin)

Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis in tumor cells.

S1225

Etoposide

Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity.

S1288

Camptothecin

Camptothecin is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Phase 2.

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.

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.

S4591New

Nitroxoline

Nitroxoline is a urinary antibacterial agent active against susceptible gram-positive and gram-negative organisms commonly found in urinary tract infections. It is a fluorquinolone that is active against bacterial gyrases.

S1228

Idarubicin HCl

Idarubicin 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.

S1223

Epirubicin HCl

Epirubicin HCl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase.

S2485

Mitoxantrone HCl

Mitoxantrone is a type II topoisomerase inhibitor with IC50 of 2.0 μM, 0.42 mM for HepG2 and MCF-7/wt cells, respectively.

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.

S1465

Moxifloxacin HCl

Moxifloxacin is a fourth-generation synthetic fluoroquinolone antibacterial agent.

S2217

Irinotecan HCl Trihydrate

Irinotecan prevents DNA from unwinding by inhibition of topoisomerase 1.

S4908

SN-38

SN-38 is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks.

S1367

Amonafide

Amonafide produces protein-associated DNA-strand breaks through a topoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage. Phase 3.

S1787

Teniposide

Teniposide is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL).

S1340

Gatifloxacin

Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.

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.

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.

S1940

Levofloxacin

Levofloxacin is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections.

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.

S1464

Marbofloxacin

Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication.

S2027

Ciprofloxacin

Ciprofloxacin is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity, with MIC90 of 0.024-6 μM.

S2492

Novobiocin Sodium

Novobiocin Sodium is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria.

S1756

Enoxacin

Enoxacin is an oral broad-spectrum fluoroquinolone antibacterial agent by inhibiting bacterial DNA gyrase and topoisomerase IV, used to treat a wide variety of infections.

S1463

Ofloxacin

Ofloxacin is a synthetic broad-spectrum antimicrobial agent.

S1509

Norfloxacin

Norfloxacin is a broad-spectrum antibiotic.

S1327

Ellagic acid

Ellagic acid has antiproliferative and antioxidant property.

S2328

Nalidixic acid

Nalidixic acid 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.

S7261

Beta-Lapachone

Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.

S4006

Clinafloxacin

Clinafloxacin is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae.

S4119

Pefloxacin Mesylate Dihydrate

Pefloxacin Mesylate Dihydrate is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication.

S2064

Balofloxacin

Balofloxacin is a quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase.

S2423

(S)-10-Hydroxycamptothecin

10-Hydroxycamptothecin is a DNA topoisomerase I inhibitor with potent anti-tumor activity.

S7518

Voreloxin (SNS-595) hydrochloride

Voreloxin is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.

S3603

Betulinic acid

Betulinic acid, a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. Phase 1/2.

S3181

Flumequine

Flumequine is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM.

Catalog No. Information Product Use Citations Product Validations
S1208

Doxorubicin (Adriamycin)

Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis in tumor cells.

S1225

Etoposide

Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity.

S1288

Camptothecin

Camptothecin is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Phase 2.

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.

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.

S4591New

Nitroxoline

Nitroxoline is a urinary antibacterial agent active against susceptible gram-positive and gram-negative organisms commonly found in urinary tract infections. It is a fluorquinolone that is active against bacterial gyrases.

S1228

Idarubicin HCl

Idarubicin 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.

S1223

Epirubicin HCl

Epirubicin HCl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase.

S2485

Mitoxantrone HCl

Mitoxantrone is a type II topoisomerase inhibitor with IC50 of 2.0 μM, 0.42 mM for HepG2 and MCF-7/wt cells, respectively.

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.

S1465

Moxifloxacin HCl

Moxifloxacin is a fourth-generation synthetic fluoroquinolone antibacterial agent.

S2217

Irinotecan HCl Trihydrate

Irinotecan prevents DNA from unwinding by inhibition of topoisomerase 1.

S4908

SN-38

SN-38 is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks.

S1367

Amonafide

Amonafide produces protein-associated DNA-strand breaks through a topoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage. Phase 3.

S1787

Teniposide

Teniposide is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL).

S1340

Gatifloxacin

Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.

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.

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.

S1940

Levofloxacin

Levofloxacin is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections.

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.

S1464

Marbofloxacin

Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication.

S2027

Ciprofloxacin

Ciprofloxacin is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity, with MIC90 of 0.024-6 μM.

S2492

Novobiocin Sodium

Novobiocin Sodium is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria.

S1756

Enoxacin

Enoxacin is an oral broad-spectrum fluoroquinolone antibacterial agent by inhibiting bacterial DNA gyrase and topoisomerase IV, used to treat a wide variety of infections.

S1463

Ofloxacin

Ofloxacin is a synthetic broad-spectrum antimicrobial agent.

S1509

Norfloxacin

Norfloxacin is a broad-spectrum antibiotic.

S1327

Ellagic acid

Ellagic acid has antiproliferative and antioxidant property.

S2328

Nalidixic acid

Nalidixic acid 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.

S7261

Beta-Lapachone

Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.

S4006

Clinafloxacin

Clinafloxacin is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae.

S4119

Pefloxacin Mesylate Dihydrate

Pefloxacin Mesylate Dihydrate is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication.

S2064

Balofloxacin

Balofloxacin is a quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase.

S2423

(S)-10-Hydroxycamptothecin

10-Hydroxycamptothecin is a DNA topoisomerase I inhibitor with potent anti-tumor activity.

S7518

Voreloxin (SNS-595) hydrochloride

Voreloxin is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.

S3603

Betulinic acid

Betulinic acid, a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. Phase 1/2.

S3181

Flumequine

Flumequine is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM.