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-173639
    AZD0516
    		Inhibitor
    AZD0516 is a first-in-class antibody-drug conjugate (ADC) targeting six-transmembrane epithelial antigen of the prostate-2 (STEAP2). The anti-STEAP2 monoclonal antibody (mAb) is conjugated via interchain cysteines to a maleimide-reactive, β-glucuronidase-cleavable linker (HY-173635) bearing the topoisomerase 1 inhibitor, Exatecan (HY-13631). AZD0516 can be used for the study of prostate cancer.
    AZD0516
  • HY-148812
    Gly-Mal-Gly-Gly-Phe-Gly-amide-methylcyclopropane-Exatecan
    		Inhibitor
    Gly-Mal-Gly-Gly-Phe-Gly-amide-methylcyclopropane-Exatecan is used for ADC Synthesis.
    Gly-Mal-Gly-Gly-Phe-Gly-amide-methylcyclopropane-Exatecan
  • HY-145513
    CL2-MMT-SN38
    		Inhibitor
    CL2-MMT-SN38 is a SN-38 derivative. SN-38, an anticancer agent, is an active metabolite of the Topoisomerase I inhibitor Irinotecan (CPT-11).
    CL2-MMT-SN38
  • HY-156403
    AuM1Phe
    		Inhibitor
    AuM1Phe, an N-Heterocyclic carbene (NHC) metal complexe, blocks the human topoisomerase I activity and actin polymerization reaction. AuM1Phe affects the growth of MDA-MB-231 breast cancer cells, with an IC50 value of 1.2 μM.
    AuM1Phe
  • HY-108876
    Daunorubicin citrate
    		Inhibitor
    Daunorubicin (Daunomycin) citrate is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin citrate inhibits DNA and RNA synthesis. Daunorubicin citrate is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin citrate is also an anthracycline antibiotic. Daunorubicin citrate can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
    Daunorubicin citrate
  • HY-146094
    Antitumor agent-63
    		Inhibitor
    Antitumor agent-63 (Compound 40), a 20 (S)-O-linked camptothecin (CPT) glycoconjugate, is an antitumor agent without toxicity towards normal cells. Antitumor agent-63 shows high stability and very weak direct topoisomerase I (Topo I) inhibition.
    Antitumor agent-63
  • 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-148668A
    MC-Gly-Gly-Phe-Gly-(S)-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-(S)-Cyclopropane-Exatecan
  • 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-174374
    Topobexin
    		Inhibitor
    Topobexin (Topobexin 9) is a highly selective inhibitor for TOP2B. Topobexin selectively inhibits TOP2B in vitro and immobilizes TOP2B on DNA. Topobexin demonstrates significant protection of cardiomyocytes against DAU-induced damage. Topobexin prevents anthracycline-induced cardiotoxicity and DAU-induced decrease in LV systolic function in vivo with rabbit model.
    Topobexin
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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