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-162101
    Topoisomerase inhibitor 3
    		Inhibitor
    Topoisomerase inhibitor 3 (compound 9) is a potent Topoisomerase inhibitor. Topoisomerase inhibitor 3 shows antiproliferative and anti-tumor activity.
    Topoisomerase inhibitor 3
  • HY-108352
    HU 331
    		Inhibitor
    HU 331 (HU 331) is a highly specific Topoisomerase II inhibitor with anticancer activity. HU 331 has shown promising inhibitory effects on human cancer cell lines in vitro and human tumor xenografts in nude mice in vivo.
    HU 331
  • HY-161980
    Topoisomerases/ribosomes-IN-1
    		Inhibitor
    Topoisomerases/ribosomes-IN-1 (compound 30f) is an inhibitor of ribosomes and topoisomerases, and has inhibitory effects on constitutively macrolide-resistant bacteria. Topoisomerases/ribosomes-IN-1 can inhibit bacterial protein synthesis (IC50: 0.647 μM) and DNA replication (IC50: 0.218 μM).
    Topoisomerases/ribosomes-IN-1
  • HY-147182
    3,6-Diamino-9(10H)-acridone
    		Inhibitor
    3,6-Diamino-9(10H)-acridone is a topoisomerase inhibitor.
    3,6-Diamino-9(10H)-acridone
  • HY-162091
    Topoisomerase I inhibitor 13
    		Inhibitor
    Topoisomerase I inhibitor 13 (Compound G11) is a Topo I inhibitor that inhibits cancer cell proliferation. Topoisomerase I inhibitor 13 significantly inhibits tumor growth in vivo.
    Topoisomerase I inhibitor 13
  • HY-157795
    Exatecan analogue 1
    		Inhibitor
    Exatecan analogue 1 (Icp-3) is a Exatecan (HY-13631) analogue. Exatecan analogue 1 can be used in the synthesis of antibody-drug conjugates (ADCs)
    Exatecan analogue 1
  • HY-181836
    IKKβ-IN-6
    		Inhibitor
    IKKβ-IN-6 is an antitumor agent. IKKβ-IN-6 inhibits IKKβ (IC50: 18.24 μM), thereby suppressing the phosphorylation of p65 and IκBα, blocking the nuclear translocation of p65, and subsequently regulating genes controlled by NF-κB. IKKβ-IN-6 also targets topoisomerase I (Topo I), induces DNA damage, ROS accumulation, loss of mitochondrial membrane potential, and S-phase arrest. IKKβ-IN-6 is applicable to related research on colorectal cancer.
    IKKβ-IN-6
  • HY-156686
    NH2-methylpropanamide-Exatecan TFA
    		Inhibitor 99.80%
    NH2-methylpropanamide-Exatecan TFA is a methylpropanamide-modified Exatecan (HY-13631), which is the common ADC Cytotoxin used in the synthesis of ADC. Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
    NH2-methylpropanamide-Exatecan TFA
  • HY-185683
    Elfetabart drozuntecan
    		Inhibitor
    Elfetabart drozuntecan (DB-1311; BNT324) is an antibody-drug conjugate (ADC) targeting B7H3. Elfetabart drozuntecan conjugates a humanized anti-B7H3 IgG1 monoclonal antibody with a topoisomerase I inhibitor via a cleavable linker. Elfetabart drozuntecan exerts antitumor activity in solid tumors. Elfetabart drozuntecan can be used for the research of advanced/metastatic solid tumors.
    Elfetabart drozuntecan
  • HY-16742R
    Gepotidacin (Standard)
    		Inhibitor
    Gepotidacin (Standard) is the analytical standard of Gepotidacin. This product is intended for research and analytical applications. Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.
    Gepotidacin (Standard)
  • HY-172395
    TopoII/tubulin-IN-1
    		Inhibitor
    TopoII/tubulin-IN-1 (Compound 1B8) is a TopoII/tubulin inhibitor. TopoII/tubulin-IN-1 can inhibit the proliferation and the level of ROS of tumor cells, induce apoptosis and cell cycle arrest of tumor cells, but has no significant cytotoxicity to normal cells. TopoII/tubulin-IN-1 has antitumor activity.
    TopoII/tubulin-IN-1
  • HY-178036
    ZM484
    		Inhibitor
    ZM484 is a potent dual p53-MDM2/TOP1 inhibitor that exhibits antiproliferative and antitumor activity both in vitro and in vivo. ZM484 effectively upregulates p53 and MDM2 proteins and maintains TOP1 inhibitory activity by the release of camptothecin (CPT) and a potent p53-MDM2 inhibitor. ZM484 induces cell cycle arrest and apoptosis by regulating the expression of key apoptosis- and cycle-related proteins, including caspase-3, Bcl-2, and Cyclin B1. ZM484 can be used for colorectal cancer research.
    ZM484
  • HY-170912
    Topo I/II-IN-2
    		Inhibitor
    Topo I/II-IN-2 (Compound 3g) is an inhibitor of Topo I and Topo II. Topo I/II-IN-2 inhibits NCI-H446 cells and NCI-H1048 cells with IC50s of 1.30 μM and 1.42 μM, respectively. Topo I/II-IN-2 induces mitochondrial Apoptosis, mitochondrial dysfunction and activity generation. Topo I/II-IN-2 inhibits the PI3K/Akt/mTOR pathway. Topo I/II-IN-2 prevents SCLC (small cell lung cancer) cell proliferation, invasion, and migration in vitro. .
    Topo I/II-IN-2
  • HY-145867
    EGFR-IN-45
    		Inhibitor
    EGFR-IN-45 is a potent epidermal growth factor receptor (EGFR) pan inhibitor, with IC50s of 0.4 µM and 1.6 µM for EGFR and CDK2, respectively. EGFR-IN-45 also inhibit Topo I and Topo II. EGFR-IN-45 arrests cancer cells in the pre-G1 phase and induces apoptosis.
    EGFR-IN-45
  • HY-RS14892
    Top1 Rat Pre-designed siRNA Set A
    		Inhibitor

    Top1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Top1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Top1 Rat Pre-designed siRNA Set A
  • HY-N19312
    Diospyrin
    		Inhibitor
    Diospyrin is a dinaphthoquinone anticancer agent with pro-apoptotic (apoptosis) activity, glutathione S-transferase (Glutathione S-transferase) inhibitory activity, and topoisomerase (Topoisomerase) I inhibitory activity. Diospyrin is present in the heartwood of various Diospyros plants and can be used for research on Ehrlich ascites carcinoma, acute myeloid leukemia, chronic myeloid leukemia, mammary adenocarcinoma, cervical epithelial carcinoma, malignant cutaneous melanoma, laryngeal epidermoid carcinoma, human osteosarcoma, and human lymphoblastic carcinoma.
    Diospyrin
  • HY-149925
    DNA Gyrase-IN-6
    		Inhibitor
    Antibacterial agent 138 is a benzothiazole inhibitor of bacterial DNA gyrase and topoisomerase IV. Antibacterial agent 138 exhibits favorable solubility and plasma protein binding. Antibacterial agent 138 has antibacterial activity against Gram-positive and Gram-negative strains. Antibacterial agent 138 is a dual GyrB and ParE inhibitor.
    DNA Gyrase-IN-6
  • HY-16562AS
    Irinotecan-d5 hydrochloride
    		Inhibitor
    Irinotecan-d5 hydrochloride is deuterated labeled Irinotecan hydrochloride (HY-16562A). Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer.
    Irinotecan-d<sub>5</sub> hydrochloride
  • HY-177688
    N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan)
    N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
    N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan)
  • HY-156517
    7Ethanol-10NH2-11F-Camptothecin
    		Inhibitor
    7Ethanol-10NH2-11F-Camptothecin is a Camptothecin (HY-16560) analogue that serves as an ADC cytotoxin for the synthesis of antibody-drug conjugates (ADCs). 7Ethanol-10NH2-11F-Camptothecin can inhibit tumor growth and is used in cancer research.
    7Ethanol-10NH2-11F-Camptothecin
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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