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-13566A
    Belotecan hydrochloride
    		Inhibitor 99.88%
    Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic camptothecin derivative.
    Belotecan hydrochloride
  • HY-16700
    PNU-159682
    		Inhibitor 98.25%
    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-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-145397
    (4-NH2)-Exatecan
    		Inhibitor 99.93%
    (4-NH2)-Exatecan, a topoisomerase inhibitor, is a derivative of Exatecan. (4-NH2)-Exatecan can be used in the synthesis of antibody-drug conjugates (ADCs) (US20200306243A1, compound A).
    (4-NH2)-Exatecan
  • 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-147270
    MC-VA-PAB-Exatecan
    		Inhibitor 99.58%
    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-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-145399
    AZ14170133
    		Inhibitor 98.78%
    AZ14170133 (SG 3932) is a Drug-Linker Conjugates for ADC, which comprises a topoisomerase inhibitor and a linker for ligand unit connecting. AZ14170133 can be used to synthesis antibody-drug conjugate (ADC).
    AZ14170133
  • 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-147271
    Mal-PEG8-Val-Ala-PAB-Exatecan
    		Inhibitor 99.48%
    Mal-PEG8-Val-Ala-PAB-Exatecan (Compound 9b) is an antibody-drug conjugate linker (ADC linker) that binds to Nectin-4 polypeptides conjugated to chemotherapeutic agents. Mal-PEG8-Val-Ala-PAB-Exatecan can be used for cancer research.
    Mal-PEG8-Val-Ala-PAB-Exatecan
  • 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-148820
    Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
    		Inhibitor 98.65%
    Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT (Formula V) is a agent-linker conjugate that composed of a potent topoisomerase I inhibitor and a linker to make an antibody agent conjugate (ADC), ABBV-969.
    Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
  • 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-A0170
    Trovafloxacin
    		Inhibitor 99.08%
    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-13562A
    Banoxantrone dihydrochloride
    		Inhibitor 99.46%
    Banoxantrone dihydrochloride is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
    Banoxantrone dihydrochloride
  • HY-17577
    Berberine chloride hydrate
    		Inhibitor 99.82%
    Berberine chloride hydrate (Natural Yellow 18 chloride hydrate) is an alkaloid that acts as an antibiotic. Berberine chloride hydrate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties.
    Berberine chloride hydrate
  • HY-13631R
    Exatecan (Standard)
    		Inhibitor
    Exatecan (Standard) is the analytical standard of Exatecan. This product is intended for research and analytical applications. Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
    Exatecan (Standard)
  • HY-N2331
    Proscillaridin A
    		Inhibitor 99.74%
    Proscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively.
    Proscillaridin A
  • HY-44369
    Exatecan Intermediate 6
    		Inhibitor 98.98%
    Exatecan Intermediate 6 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 6 can be used to synthesize Antibody-Drug Conjugates (ADCs).
    Exatecan Intermediate 6
  • HY-B0330A
    Levofloxacin hydrate
    		Inhibitor 99.93%
    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
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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