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-15753A
    Ellipticine hydrochloride
    		Inhibitor 99.34%
    Ellipticine (NSC 71795) hydrochloride is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.
    Ellipticine hydrochloride
  • HY-156617
    Cyclopropaneacetamide-Exatecan
    		Inhibitor 99.60%
    Cyclopropaneacetamide-Exatecan is an Exatecan (HY-13631) analogue and an ADC Cytotoxin. Cyclopropaneacetamide-Exatecan can be used to synthesize ADC molecules for cancer research.
    Cyclopropaneacetamide-Exatecan
  • HY-118590
    ICRF-193
    		Inhibitor 99.64%
    ICRF-193 is an TopoII inhibitor. (S,S)- and (R,R)-isomers ICRF-193 make up an racemic mixture, ICRF-196 (HY-118590A). ICRF-196 can be used for the research of cancer.
    ICRF-193
  • HY-164152A
    ADC Control Human IgG1-Deruxtecan (DAR 8)
    		Inhibitor
    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-B1099
    Hycanthone
    		Inhibitor 99.97%
    Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent.
    Hycanthone
  • HY-42487B
    (R)-Exatecan Intermediate 1
    		99.95%
    (R)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631), a camptothecin-based anticancer agent. Exatecan inhibits tumor growth by interfering with the proliferation and division of tumor cells by interacting with DNA. Exatecan is primarily used in research into a variety of cancers including ovarian, lung and breast cancer.
    (R)-Exatecan Intermediate 1
  • HY-153795
    Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan
    		Inhibitor 99.09%
    Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan is a drug-linker conjugate for ADC. Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan consists of Exatecan (HY-13631) and a linker. Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan can be used for synthesis of ADCs and for cancer research.
    Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan
  • HY-118581
    Coralyne chloride
    		Inhibitor 98.30%
    Coralyne chloride is a protoberberine alkaloid with potent anti-cancer activities. Coralyne chloride acts as a potent topoisomerase I poison and induces Top I mediated DNA cleavage. Coralyne chloride can be used for preparing?coralyne derivatives?as DNA binding fluorescent probes.
    Coralyne chloride
  • HY-148668
    MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan
    		Inhibitor
    MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan is a agent-linker conjugates for ADC, consisting Exatecan (HY-13631). Exatecan is a DNA Topoisomerase I inhibitor (IC50=2.2 μM).
    MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan
  • HY-13631J
    (1R,9R)-Exatecan mesylate
    		99.94%
    (1R,9R)-Exatecan mesylate((1R,9R)-DX8951f) is an isomer of Exatecan mesylate (HY-13631A). Exatecan mesylate (DX8951f) is an inhibitor of DNA topoisomerase I with an IC50 of 2.2 μM (0.975 μg/mL) and can be used in cancer research.
    (1R,9R)-Exatecan mesylate
  • HY-135867E
    NHC-triphosphate tetraammonium
    		Inhibitor
    NHC-triphosphate tetraammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a triphosphate form. NHC-triphosphate tetraammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA.
    NHC-triphosphate tetraammonium
  • HY-10982
    Amonafide
    		Inhibitor 99.92%
    Amonafide is a topoisomerase II inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA.
    Amonafide
  • HY-16518
    Voreloxin Hydrochloride
    		Inhibitor 99.58%
    Voreloxin Hydrochloride is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.
    Voreloxin Hydrochloride
  • HY-13551A
    Amsacrine hydrochloride
    		Inhibitor 99.92%
    Amsacrine hydrochloride (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
    Amsacrine hydrochloride
  • HY-B0067
    Amrubicin
    		Inhibitor ≥98.0%
    Amrubicin (SM-5887) is a DNA topoisomerase II inhibitor, used for the research of cancer.
    Amrubicin
  • HY-13631I
    (1S,9R)-Exatecan mesylate
    		98.48%
    (1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is an isomer of Exatecan mesylate (HY-13631A). Exatecan mesylate (DX8951f) is an inhibitor of DNA topoisomerase I with an IC50 of 2.2 μM (0.975 μg/mL) and can be used in cancer research.
    (1S,9R)-Exatecan mesylate
  • HY-13721
    Phenoxodiol
    		Inhibitor 99.89%
    Phenoxodiol (Idronoxil), a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner.
    Phenoxodiol
  • HY-13566
    Belotecan
    		Inhibitor 99.86%
    Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer.
    Belotecan
  • HY-16228
    Genz-644282
    		Inhibitor 99.13%
    Genz-644282 is a non-camptothecin topoisomerase I inhibitor, used for cancer research.
    Genz-644282
  • HY-B0455
    Lomefloxacin hydrochloride
    		Inhibitor 99.97%
    Lomefloxacin hydrochloride (NY-198 hydrochloride) is an orally active difluoroquinolone antibiotic. Lomefloxacin hydrochloride prevents DNA supercoiling and replication by inhibiting bacterial topoisomerase II. Lomefloxacin hydrochloride induces ROS production and Apoptosis. Lomefloxacin hydrochloride has broad-spectrum bactericidal activity against Gram-positive and Gram-negative bacteria. Lomefloxacin hydrochloride has anticancer effects against melanoma. Lomefloxacin hydrochloride can be used in the study of systemic bacterial infections (such as Salmonella typhimurium infections), skin and melanoma .
    Lomefloxacin hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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