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
(2)
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Topoisomerase Modulator
(1)
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Topoisomerase Inducer
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Topoisomerase Degraders
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Topoisomerase Controls
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Topoisomerase Ligands
(2)
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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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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.
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Exatecan mesylate (Standard)
0 ImagesCat. No.: HY-13631ARCAS No.: 169869-90-3Synonyms: DX8951f (Standard)Exatecan mesylate (Standard) is the analytical standard of Exatecan mesylate (HY-13631A). This product is intended for research and analytical applications. Exatecan mesylate (DX8951f) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL). Exatecan mesylate can be used in cancer research.
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Topotecan hydrochloride (Standard)
0 ImagesSynonyms: SKF 104864A hydrochloride (Standard); NSC 609669 hydrochloride (Standard)Topotecan (hydrochloride) (Standard) is the analytical standard of Topotecan (hydrochloride). This product is intended for research and analytical applications. Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.
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Anti-Trypanosoma cruzi agent-9
0 ImagesCat. No.: HY-185309CAS No.: 3094993-05-9Anti-Trypanosoma cruzi agent-9 is a topoisomerase II inhibitor. Anti-Trypanosoma cruzi agent-9 inhibits the growth of Trypanosoma cruzi and Leishmania donovani.
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ICRF 192
0 ImagesCat. No.: HY-183524CAS No.: 58893-33-7ICRF 192 is a weak DNA topoisomerase II (DNA topoisomerase II) inhibitor with an IC50 of 91 μM. ICRF 192 forms an iron-chelating derivative via ring-opening hydrolysis, which can displace Fe3+ from the Fe3+-doxorubicin complex. ICRF 192 is used for studies on the structure-activity relationship of bisdioxopiperazines and the cardiotoxicity of anthracycline drugs.
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Pefloxacin mesylate dihydrate (Standard)
0 ImagesCat. No.: HY-B0147BRCAS No.: 149676-40-4Synonyms: Pefloxacinium mesylate dihydrate (Standard)Pefloxacin (Pefloxacinium) mesylate dihydrate (Standard) is the analytical standard of Pefloxacin mesylate dihydrate (HY-B0147B). This product is intended for research and analytical applications. Pefloxacin (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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DACA (Standard)
0 ImagesCat. No.: HY-100777RCAS No.: 89459-25-6DACA (Standard) is the analytical standard of DACA (HY-100777). This product is intended for research and analytical applications. DACA (XR 5000) is a blood-brain barrier-penetrating topoisomerase I and II inhibitor. DACA can be used in the research of colorectal cancer, leukemia and lung cancer.
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Topoisomerase I-IN-22
0 ImagesCat. No.: HY-182816CAS No.: 3080330-34-0Topoisomerase I-IN-22 is an inhibitor of MRSA DNA Topoisomerase I with an IC50 of 0.85 μg/mL. Topoisomerase I-IN-22 can specifically disrupt the cell membrane structure of MRSA, enter the interior of bacteria and inhibit the activity of DNA Topoisomerase I, thereby interfering with the processes of DNA replication and transcription. Topoisomerase I-IN-22 can be used for the research of MRSA infection.
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(S)-Gyramide A
0 ImagesCat. No.: HY-116231CAS No.: 1000592-48-2(S)-Gyramide A is a weak inhibitor of cell proliferation that can target DNA gyrase.
