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-16261B
    MC-DOXHZN hydrochloride
    		Inhibitor 98.04%
    MC-DOXHZN ((E/Z)-Aldoxorubicin) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), with acid-sensitive properties.
    MC-DOXHZN hydrochloride
  • HY-100309
    9-Aminocamptothecin
    		Inhibitor 98.89%
    9-Aminocamptothecin (9-Amino-CPT) is a topoisomerase I inhibitor with potent anticancer activity.
    9-Aminocamptothecin
  • HY-N6880
    Rabdosiin
    		Inhibitor 99.55%
    Rabdosiin is a tetramer of caffeic acid isolated from the stem of Ocimum sanctum. Rabdosiin possess anti-allergic activity, anti-HIV activity and inhibition on DNA topoisomerase.
    Rabdosiin
  • HY-12930
    SPR719
    		Inhibitor 99.50%
    SPR719 (VXc-486) is an orally active gyrase B inhibitor, with bactericidal activity. SPR719 potently inhibits multiple agent-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis, with MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively. SPR719 is promising for research of lung disease caused by non-tuberculous mycobacteria (NTM).
    SPR719
  • HY-B0526
    Flumequine
    		Inhibitor 99.65%
    Flumequine (R-802) is a quinolone antibiotic, and acts as a topoisomerase II inhibitor, with an IC50 of 15 μM (3.92 μg/mL).
    Flumequine
  • 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-147095
    Val-Ala-PABC-Exatecan
    		Inhibitor 99.90%
    Val-Ala-PABC-Exatecan is a Drug-Linker Conjugates for ADC，consiting of a cleavable Tesirine linker (Val-Ala-PABC) and Exatecan (topoisomerase I inhibitor，HY-13631). Val-Ala-PABC-Exatecan can be used for ADC molecues synthesis，such as Mal-PEGn-amide-va-Exatecan.
    Val-Ala-PABC-Exatecan
  • HY-13758A
    TAS-103 dihydrochloride
    		Inhibitor 98.87%
    TAS-103 dihydrochloride is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
    TAS-103 dihydrochloride
  • HY-18351
    Indotecan
    		Inhibitor ≥98.0%
    Indotecan (LMP-400), an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis.
    Indotecan
  • HY-79490
    Ac-Exatecan
    		Inhibitor 98.70%
    Ac-Exatecan is acetylated Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM).
    Ac-Exatecan
  • 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-164792
    DBCO-PEG3-VC-Exatecan
    		Inhibitor
    DBCO-PEG3-VC-Exatecan (compound 25) is a Drug-Linker Conjugate for ADC. DBCO-PEG3-VC-Exatecan contains the ADC linker (DBCO-PEG3-VC) and a DNA topoisomerase I inhibitor Exatecan (HY-13631).
    DBCO-PEG3-VC-Exatecan
  • 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-100875A
    Bisantrene dihydrochloride
    		Inhibitor 98.86%
    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-148380A
    Mal-PEG8-Phe-Lys-PAB-Exatecan TFA
    		Inhibitor 98.44%
    Mal-PEG8-Phe-Lys-PAB-Exatecan TFA is a agent-linker conjugate for ADC, composed of degradable linker Mal-PEG8-Phe-Lys-PAB and toxin molecule Exatecan (HY-13631).
    Mal-PEG8-Phe-Lys-PAB-Exatecan TFA
  • HY-B0398A
    Nalidixic acid sodium salt
    		Inhibitor 99.83%
    Nalidixic acid sodium salt, 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.
    Nalidixic acid sodium salt
  • 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-13061
    Daun02
    		Inhibitor 98.72%
    Daun02 is a proagent of the topoisomerase inhibitor Daunorubicin.
    Daun02
  • HY-163099
    P5(PEG24)-VC-PAB-Exatecan
    		Inhibitor 99.74%
    P5(PEG24)-VC-PAB-Exatecan (LP5) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker P5(PEG24)-VC-PAB to make antibody agent conjugate (ADC). P5(PEG24)-VC-PAB-Exatecan can be used for the research of tumor.
    P5(PEG24)-VC-PAB-Exatecan
  • 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>
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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