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Topoisomerase

Topoisomerases are enzymes that participate in the overwinding or underwinding of DNA. The winding problem of DNA arises due to the intertwined nature of its double-helical structure. During DNA replication and transcription, DNA becomes overwound ahead of a replication fork.

  • Doxorubicin hydrochloride
    T102025316-40-9
    Doxorubicin hydrochloride (Adriamycin) belongs to the anthracycline class of antibiotics and is an inhibitor of human DNA topoisomerase I/II (IC50=0.8/2.67 μM). Doxorubicin hydrochloride exhibits cytotoxicity and antitumor activity. Doxorubicin hydrochloride reduces the phosphorylation of AMPK and its downstream target protein acetyl coenzyme A carboxylase, and induces apoptosis and autophagy.
    • $34
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  • Etoposide
    T013233419-42-0
    Etoposide (VP-16-213) is a topoisomerase II inhibitor that inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50=60.3 μM). Etoposide has antitumor activity and induces apoptosis and autophagy.
    • $33
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  • Sophoridine
    T33396882-68-4
    Sophoridine (Dihydro-5-episophocarpine), a natural anticancer drug, has been used in China for decades. A series of novel N-substituted Sophoridinic acid derivatives were synthesized and evaluated for their cytotoxicity with 1 as the lead. The structure-activity relationship indicated that introduction of an aliphatic acyl on the nitrogen atom might significantly enhance the anticancer activity. Among the compounds, 6b bearing bromoacetyl side-chain afforded a potential effect against four human tumor cell lines (liver, colon, breast, and lung). The mechanism of action of 6b is to inhibit the activity of DNA topoisomerase I, followed by the S-phase arrest and then cause apoptotic cell death, similar to that of its parent 1.
    • $50
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  • Exatecan Mesylate
    TQ0088169869-90-3
    Exatecan Mesylate (DX8951f) is a DNA topoisomerase I inhibitor (IC50: 2.2 μM, 0.975 μg/mL).
    • $29
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  • Berberine
    T4S07972086-83-1
    1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.
    • $50
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  • Prulifloxacin
    T5394123447-62-1
    Prulifloxacin (NM441) is a broad-spectrum fluoroquinolone antibiotic. It Inhibits bacterial DNA synthesis by inhibiting the activity of bacterial DNA topoisomerase II and IV.
    • $41
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  • Camptothecin
    T11237689-03-4
    Camptothecin (CPT) belongs to the alkaloid group of natural products and is a specific DNA topoisomerase I (Topo I) inhibitor (IC50=679 nM) with specificity. Camptothecin has antitumor activity and induces apoptosis.
    • $46
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  • EIDD-1931
    T84983258-02-4
    EIDD-1931 (Beta-d-N4-hydroxycytidine) is a ribonucleoside analog with antiviral activity.It inhibits replication of severe acute respiratory syndrome coronavirus (SARS-CoV) in Vero 76 cells, Middle East respiratory syndrome coronavirus (MERS-CoV) in Calu-3 2B4 cells, and SARS-CoV-2 in Vero cells (IC50s =0.1, 0.15 and 0.3 μM, respectively)
    • $33
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  • Berberine chloride
    T0461633-65-8
    Berberine chloride (Natural Yellow 18) is an alkaloid from Hydrastis canadensis L., Berberidaceae and also found in many other plants. It is relatively toxic to parenterally but has been used orally for various fungal and parasitic infections and an anti-diarrheal.
    • $29
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  • Ciprofloxacin monohydrochloride
    T025093107-08-5
    Ciprofloxacin monohydrochloride (Bay-09867 hydrochloride) is a broad-spectrum antimicrobial carboxyfluoroquinoline.
    • $41
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  • Norfloxacin
    T130670458-96-7
    Norfloxacin (MK-0366)(Norxacin) is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.
    • $41
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  • NU2058
    T3186161058-83-9
    NU2058 (O(6)-Cyclohexylmethylguanine) is a guanine-based CDK inhibitor, also inhibits DNA topoisomerase II ATPase activity.
    • $45
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  • Chloroquinoxaline sulfonamide
    T1495397919-22-7In house
    Chloroquinoxaline sulfonamide (Chloroquinoxaline) is a topoisomerase II alpha/beta toxin with antitumor activity and immunosuppressive properties that inhibits the proliferation of B16 melanoma cells in mice, and can be used to study metastatic colorectal cancer. It can be used to study metastatic colorectal cancer.
    • $56 TargetMol
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  • Razoxane
    T2604621416-67-1
    Razoxane is used as an antimitotic agent with immunosuppressive properties.
    • $157
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  • Bimolane
    T348174550-97-3
    Bimolane is a topoisomerase II inhibitor.
    • $35
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  • Gimatecan HCl
    T21319L In house
    Gimatecan HCl (ST1481 HCL) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.
    • $39
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  • Simmitecan hydrochloride
    T711371247847-78-4In house
    Simmitecan hydrochloride is a camptothecin derivative, a topoisomerase I inhibitor with anticancer activity, which can be used to study is solid tumors.
    • $588 TargetMol
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  • Oxaquin TEA
    T12337L In house
    Oxaquin TEA (MCB-3837 TEA), a precursor compound to MCB3681, is a DNA topoisomerase inhibitor that can be used to study Clostridium difficile infections and cross-infections.
    • $195
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  • Topovale
    T9088500214-53-9
    Topovale (ARC111) is a potent inhibitor of topoisomerase I. Topovale inhibits hypoxia-mediated accumulation of hypoxia-inducible factor-1alpha. Topovale exhibited low nM cytotoxicity against a panel of cancer cells. Topovale cytotoxicity as well as Topovale-induced apoptosis was reduced > 100-fold in CPT-resistant topoisomerase I (TOP1)-deficient P388/CPT45 cells as compared with P388 cells.
    • $88
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  • Leurubicin
    T2568870774-25-3In house
    Leurubicin (N-Leucyldoxorubicin) is a potential Top II inhibitor for the study of bacterial infections .
    • $293
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  • Daniquidone
    T6889667199-66-0In house
    Daniquidone (Batracylin) is a potent dual inhibitor of DNA topoisomerase I and DNA topoisomerase II with cytotoxic and antiproliferative activity that induces DNA fragmentation for the study of neoplasms, immune disorders, and lymphatic disorders.
    • $48
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  • F-14512
    T27299866874-63-7
    F-14512 (free base) is a topoisomerase II inhibitor for the study of acute myeloid leukemia.
    • $293
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  • Alalevonadifloxacin
    T678262892364-59-7In house
    Alalevonadifloxacin is a DNA gyrase and DNA topoisomerase inhibitor and a novel antibacterial compound of the quinolone class targeting MRSa. Alalevonadifloxacin is potentially useful in the treatment of bacterial Gram-positive, Gram-negative and anaerobic infections.
    • $210
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  • XR-11576 HCl
    T26339L In house
    XR-11576 HCl is a novel orally active dual topoisomerase I and II inhibitor with antitumor activity.
    • $195
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  • Aldoxorubicin hydrochloride
    T11090L11361563-03-2In house
    Aldoxorubicin hydrochloride is an albumin-binding prodrug of Doxorubicin, a DNA topoisomerase II inhibitor. Aldoxorubicin hydrochloride is released from albumin under acidic conditions. Aldoxorubicin hydrochloride exhibits potent antitumor activities in various cancer cell lines and in murine tumor models.
    • $57
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  • Topoisomerase II inhibitor 14
    T77650305343-00-4
    Topoisomerase II inhibitor 14 is a potent topoisomerase II inhibitor with anticancer and antioxidant activities.Topoisomerase II inhibitor 14 induces apoptosis and blocks the cell cycle in S phase.Topoisomerase II inhibitor 14 reduces the amount of GSH, MDA and NO. Topoisomerase II inhibitor 14 reduces the amount of GSH, MDA and NO.
    • $195
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  • Pegamotecan
    T24610581079-18-7In house
    Pegamotecan (PEG-camptothecin) is a topoisomerase I (TOP1) inhibitor with anticancer activity, and it is used in the treatment of esophageal, non-small cell lung and pancreatic cancers.
    • $390
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  • Tubulin inhibitor 35
    T775842247047-77-2
    Tubulin inhibitor 35 (Tubulin IN 35) is a potent dual inhibitor of topoisomerase I and microtubule protein polymerization with antitumor activity, inhibits migration and invasion of MGC-803 and RKO cell lines, interrupts the cell cycle and induces apoptosis.
    • $54
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  • XR 5944
    T35187343247-32-5
    XR 5944 is an antitumor compound that targets DNA, is a topoisomerase inhibitor, inhibits ER activity, and can be used to study colon and lung cancer.
    • $293
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  • Topixantrone 2HCl
    T28994L2514569-86-7In house
    Topixantrone 2HCl is a DNA topoisomerase inhibitor with antitumor activity for the study of gastric and prostate cancer.
    • $195
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  • (4-NH2)-Exatecan
    T401592495742-21-5In house
    (4-NH2)-Exatecan is a topoisomerase inhibitor with potential anticancer activity for the synthesis of antibody drug conjugates (ADCs).
    • $123
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  • Gimatecan
    T21319292618-32-7In house
    Gimatecan (STI481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.
    • $116
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  • DRF-1042
    T15168200619-13-2In house
    DRF-1042 is an orally active camptothecin analog with antitumor activity and inhibits DNA topoisomerase I. It is used in the study of refractory tumors.
    • $30
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  • Pyrazoloacridine
    T2847599009-20-8In house
    Pyrazoloacridine (PD 115934) is a nucleic acid binding agent that inhibits the activity of topo I and II with an IC50 of 1.25 μM in K562 cells. Pyrazoloacridine shows anti-cancer activity.
    • $36
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  • Ellipticine
    T1166519-23-3In house
    Ellipticine (Elliptisine) is a potent antineoplastic agent exhibiting multiple mechanisms of action, IC50 of 0.67±0.06, 1.25±0.13, 1.25±0.13, 0.67±0.06, 0.27±0.02, 0.49±0.04, 0.44±0.03, and 1.48±0.62 μM for Leukemia HL-60, Breast adenocarcinoma MCF-7, Breast adenocarcinoma MCF-7, Leukemia HL-60, Neuroblastoma IMR-32, Neuroblastoma UKF-NB-4, Neuroblastoma UKF-NB-3, and Glioblastoma U87 mg cell, respectively.
    • $47
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  • Amsacrine
    T120651264-14-3
    Amsacrine (AMSA) (mAMSA) an antineoplastic agent which can intercalate into the DNA of tumor cells. Amsacrine also expresses topoisomerase inhibitor activity, specifically inhibiting topoisomerase II.
    • $39
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  • β-Lapachone
    T64074707-32-8
    β-Lapachone (ARQ-501) is a specific DNA topoisomerase I inhibitor, and no inhibitory activities against DNA topoisomerase II or ligase.
    • $40
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  • Aldoxorubicin
    T11090L1361644-26-9
    Aldoxorubicin has effective antitumor activities in various cancer cell lines and in murine tumor models. Aldoxorubicin is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitors).
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  • Doxorubicin
    T145623214-92-8
    Doxorubicin (Adriamycin) is a Topoisomerase II (Top2) inhibitor with antineoplastic activity.
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  • Teniposide
    T152329767-20-2
    Teniposide (VM26), a semisynthetic derivative of podophyllotoxin with antitumor activity, inhibits DNA synthesis by forming a complex with topoisomerase II and DNA.
    • $54
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  • Epirubicin hydrochloride
    T012556390-09-1
    Epirubicin hydrochloride (Pharmorubicin) is an antineoplastic agent which can inhibit Topoisomerase.
    • $33
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  • Mitoxantrone
    T658865271-80-9
    Mitoxantrone (mitozantrone) is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Mitoxantrone is less cardiotoxic compared to doxorubicin.
    • $33
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  • Levofloxacin
    T6567100986-85-4
    Levofloxacin (Fluoroquinolone) is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections.
    • $48
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  • Betulinic acid
    T2830472-15-1
    Betulinic acid (ALS-357) is a pentacyclic lupane-type triterpene derivative of betulin (isolated from the bark of Betula alba, the common white birch) which has antiretroviral, antimalarial, and anti-inflammatory properties, as well as a more recently discovered potential as an anticancer agent, by inhibition of topoisomerase.
    • $33
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  • Ellipticine hydrochloride
    T46145081-48-1
    Ellipticine hydrochloride (NSC-71795 (hydrochloride)) is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.
    • $40
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  • Pirarubicin
    T662872496-41-4
    Pirarubicin (Theprubicin) is an anthracycline antibiotic. It is also a DNA/RNA synthesis inhibitor that intercalates into DNA and interacts with topoisomerase II, utilized as an antineoplastic agent.
    • $32
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  • Ellagic acid
    T0465476-66-4
    Ellagic acid (Gallogen) is a fused four ring compound isolated from the kino of Eucalyptus maculata Hook and E. Hemipholia F. Muell. Activates Factor XII of the blood clotting system which also causes kinin release; used in research and as a dye.
    • $44
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  • Daunorubicin hydrochloride
    T151123541-50-6
    Daunorubicin hydrochloride (Rubidomycin hydrochloride), an anthracycline aminoglycoside antineoplastic, inhibits DNA replication and repair and RNA and protein synthesis.
    • $31
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  • Ofloxacin
    T090282419-36-1
    Ofloxacin (Oxaldin) is a fluoroquinolone antibacterial antibiotic. Ofloxacin binds to and inhibits bacterial topoisomerase II (DNA gyrase) and topoisomerase IV, enzymes involved in DNA replication and repair, resulting in cell death in sensitive bacterial species.
    • $50
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  • Idarubicin hydrochloride
    T601057852-57-0
    Idarubicin hydrochloride (Zavedos), a hydrochloride salt form of Idarubicin, is a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells ( IC50: 3.3 ng/mL).
    • $55
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