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-N0716B
    Berberine sulfate
    		Inhibitor ≥98.0%
    Berberine sulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine sulfate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine sulfate has antineoplastic properties. The sulfate form improves bioavailability.
    Berberine sulfate
  • 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-W021377
    Exatecan Intermediate 2
    		Inhibitor 99.95%
    Exatecan Intermediate 2 (compound B) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers.
    Exatecan Intermediate 2
  • HY-145397
    (4-NH2)-Exatecan
    		Inhibitor ≥99.0%
    (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-N0095
    (S)-10-Hydroxycamptothecin
    		Inhibitor 99.38%
    (S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment.
    (S)-10-Hydroxycamptothecin
  • HY-103399
    Trovafloxacin mesylate
    		Inhibitor 99.56%
    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-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-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-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-145399
    Mal-PEG8-amide-Val-Ala-(4-NH2)-Exatecan
    		Inhibitor 98.95%
    Mal-PEG8-amide-Val-Ala-(4-NH2)-Exatecan is a Drug-Linker Conjugates for ADC, which comprises a topoisomerase inhibitor and a linker for ligand unit connecting. Mal-PEG8-amide-Val-Ala-(4-NH2)-Exatecan can be used to synthesis antibody-drug conjugate (ADC).
    Mal-PEG8-amide-Val-Ala-(4-NH2)-Exatecan
  • HY-13630
    Etoposide phosphate
    		Inhibitor
    Etoposide phosphate (BMY-40481) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate is the phosphate ester proagent of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate induces cell cycle arrest, apoptosis, and autophagy.
    Etoposide phosphate
  • HY-100875
    Bisantrene
    		Inhibitor 98.08%
    Bisantrene is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene targets eukaryotic type II topoisomerases. Bisantrene is a substrate of MDR1.
    Bisantrene
  • 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-13725A
    Pirarubicin Hydrochloride
    		Inhibitor 98.56%
    Pirarubicin Hydrochloride is an anthracycline antibiotics, acts as a topoisomerase II inhibitor, and is a widely used for treatment of various cancers, in particular, solid tumors.
    Pirarubicin Hydrochloride
  • HY-N2306
    Aclacinomycin A
    		Inhibitor 98.95%
    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-147271
    Mal-PEG8-Val-Ala-PAB-Exatecan
    		Inhibitor 98.75%
    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-44369
    Exatecan Intermediate 6
    		Inhibitor 98.92%
    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-13727A
    Pixantrone
    		Inhibitor 98.38%
    Pixantrone (BBR 2778) dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
    Pixantrone
  • 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
  • HY-13551
    Amsacrine
    		Inhibitor 99.95%
    Amsacrine (m-AMSA; acridinyl anisidide) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
    Amsacrine
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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