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
(748)
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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 (824)
Related Products (824)
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Recombinant Proteins (1)
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Antibodies (4)
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Topoisomerase Isoform Comparison
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Asulacrine isethionate
0 ImagesCat. No.: HY-13552CAS No.: 80841-48-1Synonyms: CI-921 isethionate; NSC 343499 isethionateAsulacrine isethionate (CI-921 isethionate) is a derivative of Amsacrine (HY-13551), a Topoisomerase II inhibitor and an anticancer agent. Asulacrine isethionate binds to DNA via intercalation, forming stable complexes with long residence times at DNA sites. Asulacrine isethionate mediates DNA breakage and DNA-protein cross-linking. Asulacrine isethionate exhibits anticancer activity against leukemia or lung cancer. Asulacrine isethionate can be used in research related to breast cancer, lung cancer, mouse solid tumors and leukemia.
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Berberine
0 ImagesBerberine (Natural Yellow 18) is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine (Natural Yellow 18) induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine (Natural Yellow 18) has antineoplastic properties. The sulfate form (HY-N0716B) improves bioavailability.
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Amonafide (Standard)
0 ImagesSynonyms: AS1413 (Standard)Amonafide (Standard) is the analytical standard of Amonafide. This product is intended for research and analytical applications. Amonafide is a topoisomerase II inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA.
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Luotonin F
0 ImagesCat. No.: HY-118726CAS No.: 244616-85-1Luotonin F is an alkaloid found in the aerial parts of the P. nigellastrum Bunge. Luotonin F shows cytotoxic activity against mouse leukemia P-388 cells by inhibiting human topoisomerase II.
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NU/ICRF 500
0 ImagesCat. No.: HY-118379CAS No.: 156074-08-7NU/ICRF 500 is a topo II catalytic inhibitor which increases CREST negative micronuclei in human lymphocytes.
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Mitoxantrone (Standard)
0 ImagesSynonyms: Mitozantrone (Standard); NSC 301739 (Standard)Mitoxantrone (Standard) is the analytical standard of Mitoxantrone. This product is intended for research and analytical applications. Mitoxantrone is a potent topoisomerase II inhibitor. Mitoxantrone also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone shows antitumor activity. Mitoxantrone also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.
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Guajadial C
0 ImagesCat. No.: HY-133219CAS No.: 1529775-02-7Guajadial C is a Top1 catalytic inhibitor that delays Top1 poison-mediated DNA damage. Guajadial C shows cytotoxicity against cancer cells.
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Pixantrone (Standard)
0 ImagesSynonyms: BBR 2778 (Standard)Pixantrone (Standard) is the analytical standard of Pixantrone. This product is intended for research and analytical applications. Pixantrone (BBR 2778) dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
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9-Hydroxyellipticin
0 ImagesCat. No.: HY-101775CAS No.: 51131-85-29-hydroxyellipticine is an inhibitor of Topo II and RyR, exhibiting high affinity for DNA with a Pka value of 9.8 at pH 7.4. It has antitumor, antioxidant, and catecholamine-releasing activities, with IC50 values of 1.6 μM and 1.2 μM for Hela S-3 and 293T cells, respectively. It also demonstrates anticancer effects in L1210 leukemia mice.
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NK 314
0 ImagesCat. No.: HY-18626CAS No.: 208237-49-4NK 314 is an inhibitor for topoisomerase IIα, which generates the break of DNA double-strand. NK 314 arrests the cell cycle at G2 phase in human acute myeloid leukemia cells, inhibits the proliferation of CEM with IC90 of 55 nM.
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Tafluposide
0 ImagesCat. No.: HY-123363CAS No.: 179067-42-6Synonyms: F-11782Tafluposide (F-11782) is a DNA topoisomerase inhibitor. Tafluposide has antitumor activity.
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Ciprofloxacin-d4
0 ImagesCat. No.: HY-B0356S2Synonyms: Bay-09867-d4Ciprofloxacin-d4 (Bay-09867-d4) is deuterium labeled Ciprofloxacin. Ciprofloxacin (Bay-09867) is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin has anti-proliferative activity and induces apoptosis. Ciprofloxacin is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
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Gatifloxacin sesquihydrate (Standard)
0 ImagesCat. No.: HY-10581CRCAS No.: 180200-66-2Synonyms: AM-1155 sesquihydrate (Standard); BMS-206584 sesquihydrate (Standard); PD135432 sesquihydrate (Standard)Gatifloxacin (sesquihydrate) (Standard) is the analytical standard of Gatifloxacin (sesquihydrate). This product is intended for research and analytical applications. Gatifloxacin sesquihydrate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin sesquihydrate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin sesquihydrate can be used to treat bacterial conjunctivitis?in vivo.
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8-Chloro-ATP
0 ImagesCat. No.: HY-134290CAS No.: 185341-71-38-Chloro-ATP, an ATP (HY-B2176) analog, is a topoisomerase II (Topo II) inhibitor. 8-Chloro-ATP inhibits DNA synthesis and induces DNA double-stranded breaks (DSBs). 8-Chloro-ATP inhibits Topo II-catalyzed ATP hydrolysis.
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(S)-Benzyl 2-cyclopropyl-2-hydroxyacetate
0 ImagesCat. No.: HY-49556CAS No.: 2414393-48-7(S)-Benzyl 2-cyclopropyl-2-hydroxyacetate is an intermediate reactant in the synthesis of Camptothecin (HY-16560). Camptothecin is an inhibitor of the DNA topoisomerase Topo I, withIC50=679 nM.
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(±)-10-Hydroxycamptothecin (Standard)
0 ImagesCat. No.: HY-N0275RCAS No.: 64439-81-2Synonyms: (±)-10-HCPT (Standard)(±)-10-Hydroxycamptothecin (Standard) is the analytical standard of (±)-10-Hydroxycamptothecin. This product is intended for research and analytical applications. (±)-10-Hydroxycamptothecin is an indole alkaloid that inhibits the activity of topoisomerase I and has a broad spectrum of anticancer activity.
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Asulacrine
0 ImagesCat. No.: HY-183480CAS No.: 80841-47-0Synonyms: CI-921; NSC 343499Asulacrine (CI-921) is an orally active DNA intercalating topoisomerase II inhibitor. Asulacrine binds to DNA via intercalation, with its acridine chromophore intercalated between base pairs and substituents located in the major/minor grooves, which stabilizes DNA against acid denaturation. Asulacrine acts as a cell cycle inhibitor, disruptor, and arrest inducer, slowing cell progression in late S/G2 phase, causing G2 phase arrest and inducing unbalanced growth. Asulacrine inhibits cell growth, clonogenicity, and colony formation, and leads to histological destruction of tumor cells. Compared to cells in exponential growth phase, Asulacrine exhibits lower toxicity to quiescent cells; its activity depends on cationic properties, and it has better water solubility and metabolic stability. Asulacrine can be used in research related to leukemia, lung cancer, colon cancer, breast cancer, melanoma, adriamycin-resistant mammary adenocarcinoma, and mouse solid tumors.
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Azithromycin-amide-C3-amide-quinoxaline
0 ImagesCat. No.: HY-180767Azithromycin-amide-C3-amide-quinoxaline (Compound 5f) is an Azithromycin (HY-17506) derivative and antibacterial agent. Azithromycin-amide-C3-amide-quinoxaline inhibits topoisoisomerase I with an IC50 of 120.7 μM. Azithromycin-amide-C3-amide-quinoxaline interacts with 70S E. coli ribosome with a Kd of 0.8 nM. Azithromycin-amide-C3-amide-quinoxaline inhibits bacterial translation with an IC50 of 0.7 μM. Azithromycin-amide-C3-amide-quinoxaline shows antibacterial potency against S. pneumonia ATCC 49619, S. aureus ATCC 29213, E. faecalis ATCC 29212 with MICs of 0.06 μg/mL, 2 μg/mL, 0.5 μg/mL, respectively. Azithromycin-amide-C3-amide-quinoxaline exhibits anticancer activity against prostate cancer, colon cancer.
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Gatifloxacin-d4
0 ImagesCat. No.: HY-W700069CAS No.: 1190043-25-4Synonyms: AM-1155-d4; BMS-206584-d4; PD135432-d4Gatifloxacin-d4 (AM-1155-d4) is the deuterium labeled Gatifloxacin (HY-10581). Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin inhibits bacterial type II topoisomerases (IC50 = 13.8 μg/mL for S. aureus topoisomerase IV) and E.coli DNA gyrase (IC50 = 0.109 μg/mL). Gatifloxacin can be used for the study of bacterial conjunctivitis in vivo.
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RPR121056 (Standard)
0 ImagesSynonyms: APC (Standard)RPR121056 (Standard) is the analytical standard of RPR121056. This product is intended for research and analytical applications. RPR121056 (APC) is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE[1].
