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
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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 (827)
Related Products (827)
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Recombinant Proteins (1)
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Antibodies (4)
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Topoisomerase Isoform Comparison
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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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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.
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TQB2102
0 ImagesCat. No.: HY-185816TQB2102 is a bispecific epitope antibody-drug conjugate targeting HER2, composed of the antibody Rolditamig (HY-P992130) and the toxin molecule Deruxtecan-d2 (HY-13631ES3). TQB2102 binds to the ECD2 and ECD4 domains of HER2, promotes its own internalization by HER2-expressing cells, and delivers deuterated DXd payload to inhibit topoisomerase I. TQB2102 induces antibody-dependent cellular cytotoxicity, DNA damage, bystander killing activity, and inhibits cancer cell proliferation. TQB2102 can be used in research related to various cancers including metastatic breast cancer, colorectal cancer, and gastric/gastroesophageal junction adenocarcinoma.
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Zocilurtatug pelitecan
0 ImagesCat. No.: HY-188059CAS No.: 3058592-88-1Synonyms: ZL-1310Zocilurtatug pelitecan (ZL-1310) is a blood-brain barrier-penetrating antibody-drug conjugate targeting DLL3. It consists of the antibody component Zocilurtatug (HY-P992148) and the toxin-linker molecule DL-01 (HY-155870). Zocilurtatug pelitecan induces cell cycle arrest and apoptosis in tumor cells, and inhibits the growth of established human tumors in xenograft models. It can be used in research on extensive-stage small cell lung cancer (SCLC) and neuroendocrine tumors.
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Aldoxorubicin hydrochloride
0 ImagesCat. No.: HY-16261CCAS No.: 1361563-03-2Synonyms: INNO-206 hydrochloride; DOXO-EMCH hydrochlorideAldoxorubicin (INNO-206) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin hydrochloride (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
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Topotecan hydrochloride hydrate
0 ImagesCat. No.: HY-13768CCAS No.: 1044663-62-8Synonyms: SKF 104864A hydrochloride hydrate; NSC 609669 hydrochloride hydrateTopotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity.
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Irinotecan liposome
0 ImagesCat. No.: HY-185371Synonyms: Irinotecan hydrochlorid liposomee; Liposomal irinotecanIrinotecan liposome is a liposome-encapsulated form of Irinotecan hydrochlorid (HY-16562A) (a topoisomerase I inhibitor). Compared with Irinotecan, Irinotecan liposome enhances antitumor activity, reduces drug release rate, and avoids neutropenia.
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Silatecan
0 ImagesCat. No.: HY-16055CAS No.: 220913-32-6Synonyms: AR-67; DB 67Silatecan (AR-67) is a blood-brain barrier-permeable derivative of Camptothecin (HY-16560), DNA topoisomerase I inhibitor, an anticancer agent, and a radiosensitizer. Silatecan potently radiosensitizes wild-type p53 gliomas. Silatecan can be used in research related to glioma, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer, breast cancer, cervical cancer, gastric cancer, nasopharyngeal cancer, and uterine cancer.
