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
(761)
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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 (838)
Related Products (838)
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Recombinant Proteins (1)
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Antibodies (4)
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Topoisomerase Isoform Comparison
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Pefloxacin mesylate dihydrate
0 ImagesSynonyms: Pefloxacinium mesylate dihydratePefloxacin (Pefloxacinium) mesylate dihydrate is a broad spectrum antibiotic. Pefloxacin mesylate dihydrate blocks DNA replication by inhibiting DNA gyrase. Pefloxacin mesylate dihydrate inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin mesylate dihydrate exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin mesylate dihydrate has anti-Plasmodium yoelii infection activity. Pefloxacin mesylate dihydrate increase UVA-induced edema and immunesuppression. Pefloxacin mesylate dihydrate can be used for infection studies.
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Bethoxazin
0 ImagesBethoxazin is a yeast DNA topoisomerase II inhibitor with an IC50 of 5.3 μM, and also a broad-spectrum industrial microbicide and covalent adduct-forming agent. Bethoxazin inhibits the catalytic activity of yeast DNA topoisomerase II by reacting with the key free cysteine thiol group on the enzyme. Bethoxazin forms covalent adducts with molecules containing free thiol groups. Bethoxazin inhibits the growth of yeast cells. Bethoxazin can be used in studies related to the growth of fungi, molds and algae.
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10NH2-11F-Camptothecin TFA
0 ImagesCat. No.: HY-156516ACAS No.: 2873461-64-210NH2-11F-Camptothecin TFA is a Camptothecin (HY-16560) analogue that serves as an ADC cytotoxin for the synthesis of antibody-drug conjugates (ADCs). 10NH2-11F-Camptothecin TFA has anticancer effects (WO2022246576A1; compound 140).
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Eupolauridine
0 ImagesCat. No.: HY-N15319CAS No.: 58786-39-3Synonyms: CanangineEupolauridine (Canangine) is a selective DNA topoisomerase II inhibitor with IC50 values of 20 μM for fungal topoisomerase I and 33 μM for human topoisomerase I. Eupolauridine exerts antifungal activity by inhibiting the catalytic activity of topoisomerase II and stabilizing its cleavage complex with DNA, leading to DNA damage. Eupolauridine is promising for research of fungal infectious diseases.
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Lurtotecan dihydrochloride
0 ImagesSynonyms: GI147211 dihydrochloride; OSI-211 dihydrochlorideLurtotecan dihydrochloride (GI147211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan dihydrochloride has anticancer effects.
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Govitecan
0 ImagesCat. No.: HY-187637CAS No.: 1918106-06-5Govitecan is a topoisomerase I inhibitor and also a linker-payload compound for antibody-drug conjugates (ADCs), with SN-38 as its active component. Govitecan serves as the linker-drug moiety of ADCs targeting CDH17-expressing cancer cells. Govitecan acts as the cytotoxic payload component of ADCs targeting Trop-2. Govitecan can be used in research related to colorectal cancer, gastric cancer, pancreatic cancer, liver cancer, metastatic triple-negative breast cancer, and other conditions.
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Topoisomerase IIα-IN-5
0 ImagesCat. No.: HY-152187CAS No.: 3037545-23-3Topoisomerase IIα-IN-5 is a topoisomerase II (topo II) α catalytic inhibitor. Topoisomerase IIα-IN-5 intercalates into DNA and binds to the DNA minor groove. Topoisomerase IIα-IN-5 exhibits better efficacy and less genotoxicity than Etoposide (HY-13629).
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7-Methoxy-9-methylfuro[2,3-b]-quinoline-4,5,8(9H)-trione
![7-Methoxy-9-methylfuro[2,3-b]-quinoline-4,5,8(9H)-trione](https://file.medchemexpress.com/product_pic/hy-169261.gif "Click to View 7-Methoxy-9-methylfuro[2,3-b]-quinoline-4,5,8(9H)-trione Product Detail")
0 ImagesCat. No.: HY-169261CAS No.: 859304-28-27-Methoxy-9-methylfuro[2,3-b]-quinoline-4,5,8(9H)-trione is a synthetic intermediate that can been used in the synthesis of the alkaloid Acronycidine.
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Viquidacin
0 ImagesCat. No.: HY-14780CAS No.: 904302-98-3Synonyms: NXL 101Viquidacin (NXL 101) is an antibiotic with inhibitory activity against topoisomerase IV and DNA gyrase. Viquidacin exhibits antibacterial activity against gram positive bacterial by inhibiting the supercoiling, decatenation and relaxation in strains Staphylococcus aureus and Escherichia coli in micromolar levels. Viquidacin inhibits S. aureus wildtype and mutants with MIC of 2-128 mg/L.
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Levofloxacin-d3 hydrochloride
0 ImagesCat. No.: HY-B0330BS1CAS No.: 1173021-78-7Synonyms: (-)-Ofloxacin-d3 hydrochlorideLevofloxacin-d3 ((-)-Ofloxacin-d3) hydrochlorideis deuterium labeled Levofloxacin (hydrochloride). Levofloxacin ((-)-Ofloxacin) hydrochloride is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrochloride inhibits the DNA gyrase and topoisomerase IV. Levofloxacin hydrochloride can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin hydrochloride shows anti-orthopoxvirus activity.
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Bakuchicin
0 ImagesBakuchicin (Allopsoralen) is a compound that can be found in Psoralea corylifolia. It has certain inhibitory activity against topoisomerase II. In the cell model infected with Simian virus 40 (SV40), the IC50 of Bakuchicin against topoisomerase II is 404 μM. Bakuchicin can be used in the research of the anti-infection field.
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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.
