Topoisomerase
Topoisomerases are enzymes that regulate the overwinding or underwinding of DNA. The winding problem of DNA arises due to the intertwined nature of its double-helical structure. Topoisomerases are isomerase enzymes that act on the topology of DNA. Type I topoisomerase cuts one strand of a DNA double helix, relaxation occurs, and then the cut strand is reannealed. Type I topoisomerases are subdivided into two subclasses: type IA topoisomerases, which share many structural and mechanistic features with the type II topoisomerases, and type IB topoisomerases, which utilize a controlled rotary mechanism. Type II topoisomerase cuts both strands of one DNA double helix, pass another unbroken DNA helix through it, and then reanneal the cut strands. This class is also split into two subclasses: type IIA and type IIB topoisomerases, which possess similar structure and mechanisms.
Topoisomerase Isoform Specific Products
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Topoisomerase Inhibitors
(769)
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Topoisomerase Agonists
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Topoisomerase Modulator
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Topoisomerase Inducer
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Topoisomerase Degraders
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Topoisomerase Controls
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Topoisomerase Ligands
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Topoisomerase Proteins
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DNA topoisomerase II Proteins
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Topoisomerase Related Products (847)
Related Products (847)
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Recombinant Proteins (1)
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Antibodies (4)
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Topoisomerase Isoform Comparison
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(1R,9R)-Exatecan
0 ImagesCat. No.: HY-13631VCAS No.: 2489613-15-0Synonyms: (1R,9R)-DX-8951(1R,9R)-Exatecan ((1R,9R)-DX8951f) is a non-prodrug Camptothecin (HY-16560) derivative and a potent topoisomerase I (Topo I) inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1R,9R)-Exatecan blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1R,9R)-Exatecan not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1R,9R)-Exatecan is widely used in preclinical studies of multiple cancers including pancreatic cancer, lung cancer, breast cancer, and leukemia. The low-activity isomer of (1R,9R)-Exatecan is (1S,9R)-Exatecan (HY-13631I).
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Gemifloxacin mesylate (Standard)
0 ImagesSynonyms: SB-265805S (Standard); LB-20304a (Standard)Gemifloxacin (mesylate) (Standard) is the analytical standard of Gemifloxacin (mesylate). This product is intended for research and analytical applications. Gemifloxacin mesylate (SB-265805S; LB-20304a) is an orally active broad-spectrum quinolone antibacterial antibiotic. Gemifloxacin mesylate inhibits DNA synthesis by inhibiting DNA gyrase and Topoisomerase IV activities. Gemifloxacin mesylate has potent antibacterial activities against gram-positive bacteria in vitro efficacy study, particularly Streptococci and Staphylococci. Gemifloxacin mesylate has been used in the research of respiratory tract infections.
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NBTI 5463
0 ImagesCat. No.: HY-172229CAS No.: 1227303-03-8NBTI 5463 is a bacterial type II topoisomerases (topoisomerase II) inhibitor with antibacterial activity. NBTI 5463 inhibits GyrA and TopoIV in Pseudomonas aeruginosa and Escherichia coli. NBTI 5463 binds to topoisomerase II to prevent DNA cleavage and religation, inhibiting bacterial DNA replication and transcription. NBTI 5463 is promising for research of Gram-negative bacterial infection.
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Gepotidacin hydrochloride
0 ImagesCat. No.: HY-16742CCAS No.: 1075235-46-9Synonyms: GSK2140944 hydrochlorideGepotidacin hydrochloride is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.
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Thaspine acetate
0 ImagesCat. No.: HY-122481CAS No.: 74578-01-1Thaspine acetate, an alkaloid, is a topoisomerase I and II inhibitor. Thaspine acetate induces cancer cell apoptosis. Thaspine acetate induces Bak and Bax activation, mitochondrial cytochrome c release and mitochondrial membrane permeabilization. Thaspine acetate can be isoalted from the cortex of the South American tree Croton lechleri.
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Belotecan (Standard)
0 ImagesSynonyms: CKD-602 free base (Standard)Belotecan (Standard) is the analytical standard of Belotecan. This product is intended for research and analytical applications. Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer.
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Antibacterial agent 229
0 ImagesCat. No.: HY-161813CAS No.: 3049500-54-8Antibacterial agent 229 (compound 8a) is a potent antibacterial agent. Antibacterial agent 229 shows antibacterial and antifungal abilities. Antibacterial agent 229 disrupts the integrity of the bacterial membrane, intercalates into DNA. Antibacterial agent 229 inhibits topoisomerase IV with an IC50 value of 10.88 µM.
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(-)-BO 2367
0 ImagesCat. No.: HY-117657CAS No.: 145902-81-4(-)-BO 2367, an antimicrobial quinolone, is a strong mammalian and bacterial topoisomerase II inhibitor. (-)-BO 2367 shows IC50 values with 3.8 μM, 0.5 μM, and 1 μM against the DNA relaxation activity of L1210 topoisomerase II and the supercoiling activities of Escherichia coli gyrase and Micrococcus luteus gyrase, respectively. (-)-BO 2367 is a potent antitumor agent.
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Topoisomerase IIα-IN-9
0 ImagesCat. No.: HY-W178011CAS No.: 16346-97-7Synonyms: 4,4'-Sulfonylbis(2-methylphenol)Topoisomerase IIα-IN-9 (NSC85582) is a bisphenol compound that has a moderate inhibitory effect on DNA topoisomerase Topoisomerase II (IC50: 571 μM). Topoisomerase IIα-IN-9 also exhibits a certain cell growth inhibitory effect, with IC50s of 117 μM and 218 μM for K562 and CHO, respectively.
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PD 0305970
0 ImagesCat. No.: HY-182417CAS No.: 351372-19-5PD 0305970 is an orally active bacterial gyrase and topoisomerase inhibitor. PD 0305970 shows exceptional activity against gram-positive and fastidious organisms and more modest activity against gram-negative species. PD 0305970 shows low spontaneous resistance frequencies. PD 0305970 shows antibacterial efficacy in murine streptococcal sepsis and pneumococcal pneumonia models. PD 0305970 can be used for the research of bacterial infection.
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Amsacrine (Standard)
0 ImagesSynonyms: m-AMSA (Standard); acridinyl anisidide (Standard)Amsacrine (Standard) is the analytical standard of Amsacrine. This product is intended for research and analytical applications. Amsacrine (m-AMSA; acridinyl anisidide) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
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AZ14170133-d5
0 ImagesCat. No.: HY-145399SSynonyms: SG 3932-d5; AZ-0133-d5AZ14170133-d5 (SG 3932-d5) is the deuterium labeled AZ14170133 (HY-145399). AZ14170133 (SG 3932) is a Drug-Linker Conjugates for ADC, which comprises a topoisomerase inhibitor and a linker for ligand unit connecting. AZ14170133 can be used to synthesis antibody-drug conjugate (ADC).
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Amsacrine lactate
0 ImagesCat. No.: HY-13551DCAS No.: 80277-11-8Synonyms: m-AMSA lactate; Acridinyl anisidide lactateAmsacrine lactate (m-AMSA lactate) is a Topoisomerase II inhibitor. Amsacrine lactate intercalates into DNA. Amsacrine lactate induces Ca2+-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine lactate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine lactate blocks HERG potassium channels in the open/inactivated state. Amsacrine lactate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine lactate exhibits anti-leukemic activity. Amsacrine lactate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine lactate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies.
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Becatecarin
0 ImagesCat. No.: HY-13565CAS No.: 119673-08-4Synonyms: NSC 655649; BMS 181176; BMY 27557Becatecarin is a rebeccamycin analog with antitumor effects. Becatecarin intercalates into DNA and inhibites the catalytic activity of topoisomerases I/II.
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8-Chloro-ATP tetrasodium
0 ImagesCat. No.: HY-134290ACAS No.: 793671-47-38-Chloro-ATP tetrasodium, an ATP (HY-B2176) analog, is a topoisomerase II (Topo II) inhibitor. 8-Chloro-ATP tetrasodium inhibits DNA synthesis and induces DNA double-stranded breaks (DSBs). 8-Chloro-ATP tetrasodium inhibits Topo II-catalyzed ATP hydrolysis.
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Antibacterial agent 236
0 ImagesCat. No.: HY-161937CAS No.: 2364479-10-5Antibacterial agent 236 (Compound 4l) is an orally active inhibitor for DNA gyrase and topoisomerase IV (IC50 is 3.2 and 300 nM in Staphylococcus aureus), and exhibits board-spectrum antibacterial activity. Antibacterial agent 236 exhibits good pharmacokinetic properties in mice.
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Nalidixic Acid-d5
0 ImagesCat. No.: HY-B0398SCAS No.: 1189467-36-4Nalidixic Acid-d5 is the deuterium labeled Nalidixic acid. Nalidixic acid, a quinolone antibiotic, is effective against both gram-positive and gram-negative bacteria. Nalidixic acid acts in a bacteriostatic manner in lower concentrations and is bactericidal in higher concentrations. Nalidixic acid inhibits a subunit of DNA gyrase and topoisomerase IV and reversibly blocks DNA replication in susceptible bacteria.
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Bisantrene dihydrochloride (Standard)
0 ImagesSynonyms: CL-216942 dihydrochloride (Standard)Bisantrene (dihydrochloride) (Standard) is the analytical standard of Bisantrene (dihydrochloride) (HY-100875A). This product is intended for research and analytical applications. Bisantrene dihydrochloride is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene dihydrochloride targets eukaryotic type II topoisomerases. Bisantrene dihydrochloride is a substrate of MDR1.
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Banoxantrone dihydrochloride (Standard)
0 ImagesSynonyms: AQ4N dihydrochloride (Standard)Banoxantrone (dihydrochloride) (Standard) is the analytical standard of Banoxantrone (dihydrochloride). This product is intended for research and analytical applications. Banoxantrone dihydrochloride is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
