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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Gly-7-MAD-MDCPT TFA
0 ImagesCat. No.: HY-132164BGly-7-MAD-MDCPT (Compound 4b) TFA is an anticancer agent. Gly-7-MAD-MDCPT TFA is a Camptothecin (HY-16560) compound, which shows cytotoxicity to various cancer cells with IC50 values of 10-1000 nM.
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SW044248
0 ImagesSW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.
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1,4-Di-tert-butylbenzene
0 ImagesCat. No.: HY-W087058CAS No.: 1012-72-21,4-Di-tert-butylbenzene is a volatile compound identified in the hexane extracts of corn cob and green millet. 1,4-Di-tert-butylbenzene shows potent inhibition against receptor proteins of Bacterial type II topoisomerase (4PLB and LpxC) in docking analysis.
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(5-Cl)-Exatecan TFA
0 ImagesCat. No.: HY-160806A(5-Cl)-Exatecan TFA is a derivative of Exatecan (HY-13631) and a DNA topoisomerase inhibitor. (5-Cl)-Exatecan TFA serves as the cytotoxic payload component in antibody-drug conjugates (ADC) targeting ROR1-positive cancers. (5-Cl)-Exatecan TFA is applicable for the research of ROR1-positive cancers.
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Pixantrone free base
0 ImagesCat. No.: HY-13727CAS No.: 144510-96-3Synonyms: BBR 2778 free basePixantrone (BBR 2778 (free base)), a mitoxantrone analog, is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
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Irinotecan (Standard)
0 ImagesSynonyms: (+)-Irinotecan (Standard); CPT-11 (Standard); VAL-413free base (Standard)Irinotecan (Standard) is the analytical standard of Irinotecan. This product is intended for research and analytical applications. Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
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Suramin sodium salt (Standard)
0 ImagesSynonyms: Suramin hexasodium salt (Standard)Suramin (sodium salt) (Standard) is the analytical standard of Suramin (sodium salt). This product is intended for research and analytical applications. Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor. Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
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Fostriecin
0 ImagesCat. No.: HY-106702ACAS No.: 87810-56-8Synonyms: PD 110161; CL 1565A; CI-920Fostriecin is a triene antibiotic. Fostriecin is a topoisomerase II and protein phosphatase PP2A inhibitor.
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Teniposide (Standard)
0 ImagesCat. No.: HY-13761RCAS No.: 29767-20-2Synonyms: VM26 (Standard)Teniposide (Standard) is the analytical standard of Teniposide. This product is intended for research and analytical applications. Teniposide is a podophyllotoxin derivative, acts as a topoisomerase II inhibitor, and used as a chemotherapeutic agent.
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Garenoxacin
0 ImagesSynonyms: BMS284756Garenoxacin (BMS284756) is an orally active quinolone antibiotic and has a broad spectrum of activity against a wide array of gram-positive and gram-negative bacteria, anaerobes, and fastidious organisms.
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Aurofusarin
0 ImagesCat. No.: HY-120805CAS No.: 13191-64-5Aurofusarin is a secondary metabolite. Aurofusarin catalytically inhibits topoisomerase II alpha, induces CYP1A1, p53, oxidative stress, DNA damage, and glutathione redox shift, intercalates into DNA, and causes S phase reduction accompanied by cytoskeletal/nuclear condensation. Aurofusarin disrupts intestinal epithelial barrier integrity, acts additively with deoxynivalenol, reduces mitochondrial activity, is cytotoxic to colon cells, and inhibits probiotic Gram-positive bacteria through outer membrane penetration without affecting Gram-negative bacteria. Aurofusarin can be used in research on colon cancer and bacterial infections.
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Nalidixic acid (Standard)
0 ImagesNalidixic acid (Standard) is the analytical standard of Nalidixic acid. This product is intended for research and analytical applications. 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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MC-DOXHZN
0 ImagesCat. No.: HY-16261ACAS No.: 151038-96-9Synonyms: (E/Z)-Aldoxorubicin; Doxorubicin(6-maleimidocaproyl)hydrazoneMC-DOXHZN ((E/Z)-Aldoxorubicin; Doxorubicin(6-maleimidocaproyl)hydrazone) is an albumin-binding proagent of Doxorubicin (HY-15142A) (DNA topoisomerase II inhibitor), with acid-sensitive properties. MC-DOXHZN can be used to synthesize ADC.
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Topovale
0 ImagesSynonyms: ARC 111Topovale (ARC 111) is a topoisomerase I inhbitor. Topovale is an antitumor agent, and shows low nM cytotoxicity against a panel of cancer cells. Topovale induces reversible topoisomerase I (TOP1) cleavage complexes in tumor cells.
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AZD5099
0 ImagesAZD5099 is an orally effective pyrrole amide inhibitor and antibacterial agent. AZD5099 shows over 10000-fold higher selectivity for bacterial type II topoisomerases than for human topoisomerase IIα, with a IC50 value of 0.032 μmol/L against Staphylococcus aureus GyrB, a IC50 of 0.760 μmol/L against Escherichia coli GyrB, a IC50 of 73 nM against Escherichia coli ParE, a Kd of 83.8 nmol/L for Staphylococcus aureus GyrB, and a IC50 of >50 μM against human topoisomerase IIα. AZD5099 inhibits rat Mrp2 ATPase activity, competitively binds to the ATP-binding site of bacterial type II topoisomerases, blocks enzyme activity, reduces bacterial DNA and RNA synthesis, disrupts DNA replication and transcription processes, and induces mitochondrial toxicity. AZD5099 exhibits activity against Gram-positive bacteria, fastidious Gram-negative bacteria and drug-resistant strains, reduces bacterial loads in mouse infection models, and has a low spontaneous resistance frequency. AZD5099 can be used in studies related to infections caused by Gram-positive bacteria and fastidious Gram-negative bacteria, methicillin-resistant Staphylococcus aureus infections, Streptococcus pneumoniae pulmonary infections, as well as Staphylococcus aureus and Escherichia coli infections.
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Berberine chloride (Standard)
0 ImagesSynonyms: Natural Yellow 18 chloride (Standard)Berberine (chloride) (Standard) is the analytical standard of Berberine (chloride). This product is intended for research and analytical applications. Berberine chloride is an alkaloid that acts as an antibiotic. Berberine chloride induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties.
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SYS6010
0 ImagesCat. No.: HY-185832SYS6010 is an antibody-drug conjugate (ADC) targeting epidermal growth factor receptor (EGFR), which is formed by conjugating the anti-EGFR humanized IgG1 monoclonal antibody Becotatug (HY-P990049) with the topoisomerase I inhibitor JS-1 (HY-178217) via a cleavable tetrapeptide linker. SYS6010 can be used in the research of advanced solid tumors such as non-small cell lung cancer.
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Datopotamab deruxtecan
0 ImagesSynonyms: DS-1062; Dato-DXdDatopotamab deruxtecan (DS-1062) is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 Kd of 0.74 nmol/L. Datopotamab deruxtecan consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer.
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Exatecan mesylate dihydrate
0 ImagesCat. No.: HY-13631PCAS No.: 197720-53-9Synonyms: DX-8951 mesylate dihydrateExatecan (DX-8951) mesylate dihydrate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
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Mitoxantrone hydrochloride liposome
0 ImagesCat. No.: HY-185372Synonyms: Liposomal mitoxantroneMitoxantrone hydrochloride liposome is a liposome-encapsulated Mitoxantrone hydrochloride (HY-13502A) (a topoisomerase II inhibitor). Compared to regular Mitoxantrone hydrochloride, Mitoxantrone hydrochloride liposome enhances antitumor activity and prolongs drug circulation time in the body.
