2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Topoisomerase

Topoisomerase

Topoisomerase

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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:

Topoisomerase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-147971
    Anticancer agent 75
    		Inhibitor
    Anticancer agent 75 is a potent anticancer agent. Anticancer agent 75 shows cytotoxicity and selectivity in cancer cell lines. Anticancer agent 75 shows cytotoxicity to normal human kidney cell lines is at least 35 times lower than that of the Doxorubicin standard. Anticancer agent 75 shows good activity of antiplasmodial.
    Anticancer agent 75
  • HY-W713570
    Nectandrin B
    		Inhibitor
    Nectandrin B is an inhibitor of DNA topoisomerases I and II, which is found in Saururus chinensis. Nectandrin B is promising for research of cancers.
    Nectandrin B
  • HY-106556
    Zorubicin
    Zorubicin (Rubidazon) is a derivative of Daunorubicin (HY-13062A). Zorubicin interacts with topoisomerase II and inhibits DNA polymerases. Zorubicin can be used for the research of acute leukemias and sarcomas.
    Zorubicin
  • HY-111047
    GSK945237
    		Inhibitor
    GSK945237 is a potent and orally active bacterial type IIA topoisomerases inhibitor. GSK945237 shows broad-spectrum activity against Gram-positive and Gram-negative bacteria (IC50 of 0.034 μg/mL against H. influenzae DNA gyrase). GSK945237 demonstrates good in vivo efficacy in a rat respiratory tract infection model. GSK945237 can be used for anti-infection research.
    GSK945237
  • HY-113642
    CP-67804
    CP-67804 is a quinolone derivative, is a topoisomerase II-targeted agent. CP-67804 effectively enhances DNA cleavage mediated by eukaryotic topoisomerase II. CP-67804 has potential as an antineoplastic agent.
    CP-67804
  • HY-155693
    Topoisomerase II inhibitor 16
    		Inhibitor
    Topoisomerase II inhibitor 16 (compound CT3) is a selective, orally active, brain-penetrant and irreversible trypanosomal topoisomerase II inhibitor by stabilizing double-stranded DNA:enzyme cleavage complexes. Topoisomerase II inhibitor 16 has the potential for Chagas disease research.
    Topoisomerase II inhibitor 16
  • HY-10581AR
    Gatifloxacin hydrochloride (Standard)
    		Inhibitor
    Gatifloxacin (hydrochloride) (Standard) is the analytical standard of Gatifloxacin (hydrochloride). This product is intended for research and analytical applications. Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride 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)[1]. Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
    Gatifloxacin hydrochloride (Standard)
  • HY-B0398AR
    Nalidixic acid sodium salt (Standard)
    		Inhibitor
    Liquiritin (Standard) is the analytical standard of Liquiritin. This product is intended for research and analytical applications. Liquiritin, a flavonoid isolated from Glycyrrhiza uralensis, is a potent and competitive AKR1C1 inhibitor with IC50s of 0.62 μM, 0.61 μM, and 3.72μM for AKR1C1, AKR1C2 and AKR1C3, respectively. Liquiritin efficiently inhibits progesterone metabolism mediated by AKR1C1 in vivo. Liquiritin acts as an antioxidant and has neuroprotective, anti-cancer and anti-inflammatory activity.
    Nalidixic acid sodium salt (Standard)
  • HY-118590A
    ICRF-196
    ICRF-196 is an racemic mixture of the (S,S)- and (R,R)-isomers of ICRF-193 (HY-118590). ICRF-193 is a DNA Topoisomerase II inhibitor. ICRF-193 can inhibit DNA syntheses and induces apoptosis. ICRF-193 exhibits anti-cancer and anti-inflammation effects. ICRF-193 shows cardioprotective effect against anthracycline toxicity to cardiomyocytes. ICRF-193 can be used for the researches of cancer, infection, inflammation and cardiovascular disease, such as acute promyelocytic leukemia.
    ICRF-196
  • HY-P10765
    DTS-108
    		Inhibitor
    DTS-108 is a prodrug of SN38 (HY-13704) (a Topoisomerase I inhibitor). DTS-108 is a conjugate generated by linking SN38 to a human oligopeptide via an esterase sensitive cross-linker. DTS-108 exhibits anti-tumor activity against colorectal, lung, and mammary cancer.
    DTS-108
  • HY-W040298R
    Ciprofloxacin lactate (Standard)
    		Inhibitor
    Ciprofloxacin (lactate) (Standard) is the analytical standard of Ciprofloxacin (lactate). This product is intended for research and analytical applications. Ciprofloxacin (Bay-09867) lactate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin lactate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin lactate has anti-proliferative activity and induces apoptosis. Ciprofloxacin lactate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity[4].
    Ciprofloxacin lactate (Standard)
  • HY-B0330AR
    Levofloxacin hydrate (Standard)
    		Inhibitor
    Levofloxacin (hydrate) (Standard) is the analytical standard of Levofloxacin (hydrate). This product is intended for research and analytical applications. Levofloxacin hydrate (Levofloxacin hemihydrate) is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrate inhibits the DNA gyrase and topoisomerase IV. Levofloxacin hydrate can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin hydrate shows anti-orthopoxvirus activity.
    Levofloxacin hydrate (Standard)
  • HY-N0872R
    Isosteviol (Standard)
    		Inhibitor
    Isosteviol (Standard) is the analytical standard of Isosteviol. This product is intended for research and analytical applications. Isosteviol ((-)-Isosteviol) is a derivative of Stevioside through acid catalyzed hydrolysis of Stevioside. Isosteviol inhibits DNA polymerase and DNA topoisomerase and has antibacterial, anticancer and anti-tuberculosis effects.
    Isosteviol (Standard)
  • HY-149238
    Topo II/HDAC-IN-1
    		Inhibitor
    Topo II/HDAC-IN-1 (7d) exhibits excellent dual inhibitory activities against Topo II and HDAC. Topo II/HDAC-IN-1 (8d) induces apoptosis.
    Topo II/HDAC-IN-1
  • HY-13727B
    Pixantrone hydrochloride
    		Inhibitor
    Pixantrone (BBR 2778 (free base)) hydrochloride, a mitoxantrone analog, is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
    Pixantrone hydrochloride
  • HY-W278582
    Topoisomerase II inhibitor 14
    		Inhibitor 99.68%
    Topoisomerase II inhibitor 14 is a potent topoisomerase II inhibtor. Topoisomerase II inhibitor 14 induces apoptosis and arrests cell cycle at S phase and G2-M phases. Topoisomerase II inhibitor 14 exhibits antioxidant effect and decreases the level of GSH, MDA, and NO. Topoisomerase II inhibitor 14 can be used for the study of neck squamous cell carcinoma (HNSCC).
    Topoisomerase II inhibitor 14
  • HY-150044
    Type II topoisomerase inhibitor 1
    		Inhibitor
    Type II topoisomerase inhibitor 1 is a potent and selective E. coli DNA gyrase inhibitor (IC50: 1.7 nM), and forms hydrogen bonds with Asp73 residue. Type II topoisomerase inhibitor 1 inhibits topoisomerase IV activity (IC50: 0.98 μM). Type II topoisomerase inhibitor 1 can be used in the research of antibacterial area.
    Type II topoisomerase inhibitor 1
  • HY-143280
    Topoisomerase II inhibitor 4
    		Inhibitor
    Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect.
    Topoisomerase II inhibitor 4
  • HY-16568R
    Irinotecan hydrochloride trihydrate (Standard)
    		Inhibitor
    Irinotecan (hydrochloride trihydrate) (Standard) is the analytical standard of Irinotecan (hydrochloride trihydrate). This product is intended for research and analytical applications. Irinotecan hydrochloride trihydrate ((+)-Irinotecan hydrochloride trihydrate) is a topoisomerase I inhibitor with antitumor activity.
    Irinotecan hydrochloride trihydrate (Standard)
  • HY-13768D
    Topotecan acetate
    		Inhibitor
    Topotecan acetate is a topoisomerase inhibitor.
    Topotecan acetate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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