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-17460A
    Garenoxacin Mesylate hydrate
    		Inhibitor 99.95%
    Garenoxacin (BMS284756) Mesylate hydrate 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.
    Garenoxacin Mesylate hydrate
  • HY-B0063
    Gimatecan
    		Inhibitor 99.28%
    Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.
    Gimatecan
  • HY-B1050
    Gemifloxacin mesylate
    		Inhibitor 99.66%
    Gemifloxacin mesylate (SB-265805S; LB-20304a) is an orally active broad-spectrum quinolone antibacterial antibiotic. Gemifloxacin mesylate inhibits DNA synthesis by inhibiting DNA gyrase and Topoisomerase IV activities. Gemifloxacin mesylate has potent antibacterial activities against gram-positive bacteria in vitro efficacy study, particularly Streptococci and Staphylococci. Gemifloxacin mesylate has been used in the research of respiratory tract infections.
    Gemifloxacin mesylate
  • HY-106031
    F-14512
    		Inhibitor 98.04%
    F-14512 is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 can be used to study breast cancer.
    F-14512
  • HY-B0356R
    Ciprofloxacin (Standard)
    		Inhibitor
    Ciprofloxacin (Standard) is the analytical standard of Ciprofloxacin. This product is intended for research and analytical applications. 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.
    Ciprofloxacin (Standard)
  • HY-10529R
    Betulinic acid (Standard)
    		Inhibitor
    Betulinic acid (Standard) is the analytical standard of Betulinic acid. This product is intended for research and analytical applications. Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties. Betulinic acid can cross the blood-brain barrier.
    Betulinic acid (Standard)
  • HY-43564
    Exatecan Intermediate 5
    		Inhibitor 99.98%
    Exatecan Intermediate 5 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 5 can be used to synthesize Antibody-Drug Conjugates (ADCs).
    Exatecan Intermediate 5
  • HY-137466
    ARN-21934
    		Inhibitor 98.02%
    ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research.
    ARN-21934
  • HY-100875A
    Bisantrene dihydrochloride
    		Inhibitor 98.85%
    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.
    Bisantrene dihydrochloride
  • HY-U00248A
    LMP744 hydrochloride
    		Inhibitor 99.08%
    LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
    LMP744 hydrochloride
  • HY-100620
    RPR121056
    		Inhibitor 99.88%
    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.
    RPR121056
  • HY-18350
    Indimitecan
    		Inhibitor 98.30%
    Indimitecan (LMP776) is a topoisomerase I (Top1) inhibitor with anticancer activities.
    Indimitecan
  • HY-106662
    Chloroquinoxaline sulfonamide
    		Inhibitor 99.06%
    Chloroquinoxaline sulfonamide (Chloroquinoxaline), a structural analogue of sulfaquinoxaline, is a topoisomerase II alpha/beta poison. Chloroquinoxaline sulfonamide is used to control coccidiosis in poultry, rabbit, sheep, and cattle. Antitumor activity.
    Chloroquinoxaline sulfonamide
  • HY-N12445
    Quercetin-3'-O-glucoside
    		Inhibitor 98.48%
    Quercetin-3'-O-glucoside is an orally active flavonoid glycoside. Quercetin-3'-O-glucoside reduces liver glucose-6-phosphatase activity, alters serum insulin and glucose levels, and regulates the activities of antioxidant enzymes in the liver and kidney. Quercetin-3'-O-glucoside inhibits DNA topoisomerase II, induces S-phase cell cycle arrest and caspase-3-mediated apoptosis in hepatocellular carcinoma cells. Quercetin-3'-O-glucoside selectively inhibits EGFR-mediated signaling pathways targeting AKT, ERK1/2, FAK and MEK1/2. Quercetin-3'-O-glucoside inhibits growth factor-induced migration and invasion in pancreatic cancer cells. Quercetin-3'-O-glucoside exerts free radical scavenging effects. Quercetin-3'-O-glucoside is applicable to research related to pancreatic cancer, diabetes, hepatocellular carcinoma and malignant tumors.
    Quercetin-3'-O-glucoside
  • HY-42487S
    Exatecan Intermediate 1-d5
    		Inhibitor 99.90%
    Exatecan Intermediate 1-d5 is the deuterium labeled Exatecan Intermediate 1.
    Exatecan Intermediate 1-d<sub>5</sub>
  • HY-16562S1
    Irinotecan-d10 hydrochloride
    		Inhibitor 99.76%
    Irinotecan-d10 (hydrochloride) is the deuterium labeled Irinotecan. Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
    Irinotecan-d<sub>10</sub> hydrochloride
  • HY-N2198
    Podocarpusflavone A
    		Inhibitor 99.62%
    Podocarpusflavone A is a biflavonoid present in the leaves of Podocarpus henkelii, with anti-tumor, topoisomerase I inhibitory, antibacterial and antifungal activities. Podocarpusflavone A exhibits antibacterial activity against Enterococcus faecalis and Pseudomonas aeruginosa. Podocarpusflavone A shows weak activity against fungal pathogens. Podocarpusflavone A targets topoisomerase I and induces cell cycle arrest and apoptosis in MCF-7 cells. Podocarpusflavone A can be used for studies on cancer, bacterial and fungal infections.
    Podocarpusflavone A
  • HY-N0275
    (±)-10-Hydroxycamptothecin
    		Inhibitor 99.57%
    (±)-10-Hydroxycamptothecin is an indole alkaloid that inhibits the activity of topoisomerase I and has a broad spectrum of anticancer activity.
    (±)-10-Hydroxycamptothecin
  • HY-10581A
    Gatifloxacin hydrochloride
    		Inhibitor 99.94%
    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). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
    Gatifloxacin hydrochloride
  • HY-101647
    Intoplicine
    		Inhibitor 98.36%
    Intoplicine (RP 60475), an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA.
    Intoplicine
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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