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-16742
    Gepotidacin
    		Inhibitor 99.92%
    Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.
    Gepotidacin
  • HY-13761
    Teniposide
    		Inhibitor 99.00%
    Teniposide is a podophyllotoxin derivative, acts as a topoisomerase II inhibitor, and used as a chemotherapeutic agent.
    Teniposide
  • HY-171945
    Telisotuzumab Adizutecan
    		Inhibitor 99.63%
    Telisotuzumab Adizutecan (ABBV-400) is an anti-c-Met antibody-drug conjugate (ADC). Telisotuzumab Adizutecan is composed of the humanized anti-c-Met antibody Telisotuzumab (HY-P99391) and the topoisomerase 1 inhibitor (7-MAD-MDCPT) (HY-132162). Telisotuzumab Adizutecan exhibits significant anti-tumor activity against advanced solid tumors such as colorectal cancer, gastric cancer, and non-small cell lung cancer.
    Telisotuzumab Adizutecan
  • HY-A0170
    Trovafloxacin
    		Inhibitor 99.43%
    Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1.
    Trovafloxacin
  • HY-164152A
    ADC Control Human IgG1-Deruxtecan (DAR 8)
    		Inhibitor 99.32%
    ADC Control Human IgG1-Deruxtecan (DAR 8) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E).
    ADC Control Human IgG1-Deruxtecan (DAR 8)
  • HY-16700
    PNU-159682
    		Inhibitor 98.50%
    PNU-159682, a metabolite of the anthracycline Nemorubicin, is a highly potent DNA topoisomerase II inhibitor with excellent cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 can be used in EDV-nanocell technology to overcome agent resistance.
    PNU-159682
  • HY-147270
    MC-VA-PAB-Exatecan
    		Inhibitor 99.01%
    MC-VA-PAB-Exatecan is a agent-linker conjugate for ADC. MC-VA-PAB-Exatecan contains the ADC linker (peptide MC-VA-PAB) and a DNA topoisomerase I inhibitor Exatecan (HY-13631). MC-VA-PAB-Exatecan synthesized ADC shows good antitumor activity.
    MC-VA-PAB-Exatecan
  • HY-13062A
    Daunorubicin
    		Inhibitor 99.94%
    Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
    Daunorubicin
  • HY-16261
    Aldoxorubicin
    		Inhibitor
    Aldoxorubicin (INNO-206) is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
    Aldoxorubicin
  • HY-16568
    Irinotecan hydrochloride trihydrate
    		Inhibitor 99.89%
    Irinotecan hydrochloride trihydrate ((+)-Irinotecan hydrochloride trihydrate) is a topoisomerase I inhibitor with antitumor activity.
    Irinotecan hydrochloride trihydrate
  • HY-B0398
    Nalidixic acid
    		Inhibitor 99.97%
    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.
    Nalidixic acid
  • HY-122575
    Aurintricarboxylic acid
    		Inhibitor
    Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway. Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM. Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM.
    Aurintricarboxylic acid
  • HY-164152
    ADC Control Human IgG1-Deruxtecan (DAR 4)
    		Inhibitor
    ADC Control Human IgG1-Deruxtecan (DAR 4) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E).
    ADC Control Human IgG1-Deruxtecan (DAR 4)
  • HY-N2306
    Aclacinomycin A
    		Inhibitor 99.30%
    Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis.
    Aclacinomycin A
  • HY-B0356B
    Ciprofloxacin hydrochloride monohydrate
    		Inhibitor 99.88%
    Ciprofloxacin (Bay-09867) hydrochloride monohydrate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin hydrochloride monohydrate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin hydrochloride monohydrate has anti-proliferative activity and induces apoptosis. Ciprofloxacin hydrochloride monohydrate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
    Ciprofloxacin hydrochloride monohydrate
  • HY-B0330A
    Levofloxacin hydrate
    		Inhibitor 99.98%
    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
  • HY-103399
    Trovafloxacin mesylate
    		Inhibitor 99.76%
    Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1.
    Trovafloxacin mesylate
  • HY-153892
    Gly-Mal-GGFG-Deruxtecan 2-hydroxypropanamide
    		Inhibitor 99.79%
    Gly-Mal-GGFG-Deruxtecan 2-hydroxypropanamide is the drug-linker conjugate for ADC, containing ADC linker Gly-Mal-GGFG and ADC cytotoxin Deruxtecan 2-hydroxypropanamide.
    Gly-Mal-GGFG-Deruxtecan 2-hydroxypropanamide
  • HY-13624
    Epirubicin
    		Inhibitor 99.31%
    Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
    Epirubicin
  • HY-145397
    (4-NH2)-Exatecan
    		Inhibitor 99.93%
    (4-NH2)-Exatecan (compound A), a topoisomerase inhibitor, is a derivative of Exatecan. (4-NH2)-Exatecan can be used in the synthesis of antibody-drug conjugates (ADCs).
    (4-NH2)-Exatecan
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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