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-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-156617A
    (αR)-Cyclopropaneacetamide-Exatecan
    		Inhibitor 99.93%
    (αR)-Cyclopropaneacetamide-Exatecan (compound 2-A), an Exenotecan derivative, is a cytotoxic agent. (αR)-Cyclopropaneacetamide-Exatecan inhibits U87MG and SK-BR-3 cells proliferation, with IC50s of 8.11 and 2.31 μM.
    (αR)-Cyclopropaneacetamide-Exatecan
  • HY-N0354
    Anthraquinone
    		Inhibitor 99.12%
    Anthraquinone is used as a precursor for dye formation and agrochemicals, existing in different organisms, such as bacteria, fungi, plants, and some animals. Anthraquinone has biological activities: anticancer, antiinflammatory, diuretic, antiarthritic, antifungal, antibacterial, antimalarial and antioxidant. Anthraquinone also plays an important role in the primary metabolism of plants by acting on the electron transport chain through the inhibition of energy transfer in the photosynthetic process. Anthraquinone can intercalates into DNA and inhibits the topoisomerase II (topo II) enzyme, resulting in cell death via Apoptosis.
    Anthraquinone
  • HY-W046353
    2-Methoxycinnamaldehyde
    		Inhibitor 98.95%
    2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound that can be isolated from Cinnamomum cassia. 2-Methoxycinnamaldehyde inhibits topoisomerase-I/II and NF-κB signaling pathway, causes mitochondrial dysfunction, induces lysosomal vesiculation, thereby leading to DNA damage and cell apoptosis. 2-Methoxycinnamaldehyde exhibits antitumor effects.
    2-Methoxycinnamaldehyde
  • 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-N3488
    Isodiospyrin
    		Inhibitor 99.77%
    Isodiospyrin, a natural dimeric naphthoquinone, is a human DNA topoisomerase I (Topoisomerase) inhibitor. Isodiospyrin can prevent both DNA relaxation and kinase activities of human topoisomerase I. Isodiospyrin shows anticancer, antibacterial and antifungal activities.
    Isodiospyrin
  • HY-156748
    MC-PEG2-VA-PAB-Exatecan
    		Inhibitor 99.61%
    MC-PEG2-VA-PAB-Exatecan (Compound DL-18) is a Drug-Linker Conjugates for ADC. MC-PEG2-VA-PAB-Exatecan consists of Exatecan (HY-13631) and a linker. MC-PEG2-VA-PAB-Exatecan can be used for synthesis of ADCs.
    MC-PEG2-VA-PAB-Exatecan
  • HY-B1050
    Gemifloxacin mesylate
    		Inhibitor 99.76%
    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-13061
    Daun02
    		Inhibitor 98.72%
    Daun02 is a proagent of the topoisomerase inhibitor Daunorubicin.
    Daun02
  • 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-17028
    Besifloxacin Hydrochloride
    		Inhibitor 98.49%
    Besifloxacin Hydrochloride is a fourth generation fluoroquinolone antibiotic. Besifloxacin Hydrochloride is a DNA gyrase and topoisomerase IV inhibitor. Besifloxacin Hydrochloride has broad-spectrum antibacterial activity, it is effective against Gram-negative and Gram-positive aerobic and anaerobic strains and reduces the incidence of drug resistance. Besifloxacin Hydrochloride has anti-inflammatory activity. Besifloxacin Hydrochloride can be used in bacterial conjunctivitis research.
    Besifloxacin Hydrochloride
  • HY-13744
    Rubitecan
    		Inhibitor 99.23%
    Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells.
    Rubitecan
  • HY-W010800A
    Cholesterol hemisuccinate Tris salt
    		Inhibitor ≥98.0%
    Cholesterol hemisuccinate Tris salt (CHS-Tris) is a with hepatoprotective an anticancer activity. Cholesterol hemisuccinate Tris salt inhibits Acetaminophen (AAP, HY-66005) hepatotoxicity, and prevents AAP-induced hepatic apoptosis and necrosis. Cholesterol hemisuccinate Tris salt inhibits DNA polymerase and DNA topoisomerase to inhibit DNA replication and repair and cell division. Thus, Cholesterol hemisuccinate Tris salt inhibits tumor growth.
    Cholesterol hemisuccinate Tris salt
  • HY-157813
    2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan
    		Inhibitor 98.27%
    2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan is a drug-linker conjugates for ADC, consiting of a cleavable linker and Exatecan (HY-13631). 2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan can be linked to anti-Her3 antibody.
    2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan
  • HY-159783
    Mal-Exatecan
    		Inhibitor 99.39%
    Mal-Exatecan is a Mal (Maleimide) modified Exatecan (HY-13631), a DNA topoisomerase I (topoisomerase I) inhibitor.
    Mal-Exatecan
  • 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-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-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-143692
    SQDG
    		Inhibitor ≥99.0%
    SQDG inhibits topoisomerase I and P-selectin receptor, exhibits anti-inflammatory, antiviral and antitumor activities. SQDG is a glycolipid that possesses sugar moieties in their head groups. SQDG is a membrane lipid that can be used to investigate the effects of structural lipid in LNP formulations.
    SQDG
  • HY-U00248
    LMP744
    		Inhibitor 98.85%
    LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
    LMP744
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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