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-B0330C
    Levofloxacin sodium
    		Inhibitor
    Levofloxacin ((-)-Ofloxacin) sodium is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin sodium inhibits the DNA gyrase and topoisomerase IV. Levofloxacin sodium can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin sodium shows anti-orthopoxvirus activity.
    Levofloxacin sodium
  • HY-107133
    Simmitecan hydrochloride
    		Inhibitor
    Simmitecan hydrochloride, a 9-substituted lipophilic Camptothecin (HY-16560) derivative, is a potent topoisomerase I inhibitor. Simmitecan hydrochloride is an anticancer agent.
    Simmitecan hydrochloride
  • HY-13768S
    Topotecan-d5
    Topotecan-d5 is the deuterium labeled Topotecan. Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95±0.24 μM of GSCs-U87.
    Topotecan-d<sub>5</sub>
  • HY-16055
    Silatecan
    		Inhibitor
    Silatecan (AR-67; DB 67) is a Camptothecin (HY-16560) analogue with improved stability and lipophilicity. Silatecan is an inhibitor for topoisomerase I, that inhibits the DNA replication and transcription, and exhibits antitumor and radiosensitizing activities
    Silatecan
  • HY-B0526R
    Flumequine (Standard)
    		Inhibitor
    Flumequine (Standard) is the analytical standard of Flumequine. This product is intended for research and analytical applications. Flumequine (R-802) is a quinolone antibiotic, and acts as a topoisomerase II inhibitor, with an IC50 of 15 μM (3.92 μg/mL).
    Flumequine (Standard)
  • HY-169509
    Topoisomerase I/II inhibitor 8
    		Inhibitor
    Topoisomerase I/II Inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of Topoisomerase I/II, capable of inducing DNA damage and PARP-1 activation, which subsequently leads to the activation of RIPK1, RIPK3, and MLKL, ultimately triggering necroptosis. Topoisomerase I/II Inhibitor 8 demonstrates remarkable anticancer activity by effectively targeting the nuclei of cancer cells and inducing cell death through necroptosis, showing great clinical potential in circumventing drug resistance in cancer treatment.
    Topoisomerase I/II inhibitor 8
  • HY-121866
    CP-84364
    		Inhibitor
    Hippeastrine hydrobromide is an active alkaloid that exhibits a good dose-dependent inhibitory effect on topoisomerase I (Top I) with an IC50 of 7.25 μg/mL. Hippeastrine hydrobromide exhibits antiproliferative and anticancer activities.
    CP-84364
  • HY-123393
    PNU-142586
    		Inhibitor
    PNU-142586 is the major metabolite of Linezolid (HY-10394). PNU-142586 can inhibit the activity of DNA topoisomerase 2-α (TOP2A) and DNA topoisomerase 2-β (TOP2B). PNU-142586 interferes with DNA replication and transcription by blocking the binding of DNA to TOP2 and inhibiting ATP hydrolysis. PNU-142586 can be used to study Linezolid-induced hematotoxicity and its molecular mechanism.
    PNU-142586
  • HY-144769
    SDOX
    		Inhibitor
    SDOX is the Doxorubicin (DOX) proagent. The loaded DOX proagents (SDOX) which can release the parent agents DOX triggered by excessive GSH in tumor cells, minimize the unexpected side effects on normal tissues without compromising the potency.
    SDOX
  • HY-175171
    Anticancer agent 276
    		Inhibitor
    Anticancer agent 276 (Compound 5) is a multi-target anticancer agent. Anticancer agent 276 has a potent anticancer activity against human tumor cells with IC50s of 6.90 and 4.48 μM for HEPG2 and MCF7 cells, respectively. Anticancer agent 276 shows strong and stable interactions across multiple targets, including Topoisomerase II, VEGFR2, c-Met, EGFR and ERα.
    Anticancer agent 276
  • HY-158388
    Anticancer agent 215
    		Inhibitor
    Anticancer agent 215 (1) is a Camptothecin compound, with IC50 values of 5.2 nM and 8.2 nM in MCF-7 cells and MDA-MB-231 cells, respectively.
    Anticancer agent 215
  • HY-16560B
    (R)-Camptothecin
    		Control
    (R)-Camptothecin is an enantiomer of Camptothecin (CPT), is inactive as an inhibitor of the DNA religation reaction and consequently do not poison Top1.
    (R)-Camptothecin
  • HY-RS14891
    Top1 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Top1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Top1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Top1 Mouse Pre-designed siRNA Set A
  • HY-146189
    Topoisomerase II inhibitor 9
    		Inhibitor
    Topoisomerase II inhibitor 9 (Compound 19b) is a Topo II inhibitor with an IC50 of 0.97 μM. Topoisomerase II inhibitor 9 is also a classical DNA-intercalator with an IC50 of 43.51 μM. Topoisomerase II inhibitor 9 arrests the cell cycle at the G2/M phase and induces apoptosis in Hep G‐2 cells.
    Topoisomerase II inhibitor 9
  • HY-175700
    YCJ-02
    		Inhibitor
    YCJ-02 is a selective Topoisomerase I (Top I) inhibitor. YCJ-02 can inhibit cell proliferation and induce apoptosis and G2/M phase arrest. YCJ-02 can induce DNA damage and increaseγ-H2AX levels. YCJ-02 can promote Top I deqradation via a ubiquitin/26S proteasome pathway. YCJ-02 increases the expressions of pro-apoptotic proteins Bad, Bax, and cleaved caspase-3. YCJ-02 shows broad-spectrum antitumor activity. YCJ-02 can be used for the research of cancer, such as intrahepatic cholangiocarcinoma (ICC).
    YCJ-02
  • HY-156516
    10NH2-11F-Camptothecin
    		Inhibitor
    10NH2-11F-Camptothecin is a Camptothecin (HY-16560) analogue that serves as an ADC cytotoxin for the synthesis of antibody-drug conjugates (ADCs). 10NH2-11F-Camptothecin can inhibit tumor growth and is used in cancer research.
    10NH2-11F-Camptothecin
  • HY-150685
    Topo I/COX-2-IN-1
    		Inhibitor
    Topo I/COX-2-IN-1 (1H-30) is a potential Topo I/COX-2 inhibitor. Topo I/COX-2-IN-1 inhibits COX-2 and Topo I with the IC50 value of 0.24 μM and 4.42 μM, respectively. Topo I/COX-2-IN-1 can induce apoptosis and inhibit migration of cancer cells, has anti-cancer activity.
    Topo I/COX-2-IN-1
  • HY-19437
    Bimolane
    		Inhibitor
    Bimolane (AT-1727), a human topoisomerase II inhibitor, can be used as an anti-neoplastic agent and for the research of psoriasis. Bimolane shows leukemogenic activity and induces multiple types of chromosomal aberrations in human lymphocytes.
    Bimolane
  • HY-176762
    TOP3B-IN-1
    		Inhibitor
    TOP3B-IN-1 (NSC-260610) is a Topoisomerase IIIβ (TOP3B) inhibitor. TOP3B-IN-1 fails to induce the formation of TOP3B cleavage complexes (TOP3Bccs) with both DNA and RNA, and destabilizes TOP3Bccs. TOP3B-IN-1 can be used as a control compound for the development of inhibitors targeting TOP3B.
    TOP3B-IN-1
  • HY-125930A
    T-2513 hydrochloride
    		Inhibitor
    T-2513 hydrochloride is a selective topoisomerase I inhibitor. T-2513 hydrochloride binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death.
    T-2513 hydrochloride
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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