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-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-179152
    Apoptosis inducer 54
    Apoptosis inducer 54 is an apoptosis inducer that interacts with topoisomerase II-DNA. Apoptosis inducer 54 induces cell cycle arrest at the S phase in cancer cells. Apoptosis inducer 54 significantly induces early and late apoptosis in A549 cells. Topoisomerase I-IN-20 can be used for the research of lung cancer and colon cancer.
    Apoptosis inducer 54
  • HY-171946
    TGA-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
    		Inhibitor
    TGA-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT is a drug-linker conjugate for ADC. TGA-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT consists of a topoisomerase 1 inhibitor (Topi MF-6) (HY-175203) and a cleavable linker (Maleimide-Ph(3,5-F)-PEG4-Val-Ala) (HY-175218). TGA-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT can be used for synthesis of ADCs.
    TGA-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
  • HY-N17442
    Echinoside A
    		Inhibitor
    Echinoside A is a saponin. Echinoside A can be isolated from sea cucumber. Echinoside A inhibits the catalytic activity of Top2α, reduces the noncovalent binding of Top2α to DNA. Echinoside A activates Caspase-3 and induces PARP cleavage. Echinoside A induces Apoptosis. Echinoside A has anticancer activity against prostate cancer, hepatocellular carcinoma, and S-180 sarcoma. Echinoside A exhibits antifungal activity against a variety of fungi, with a minimum growth inhibitory concentration range of 3.12 to 50.0 μg/mL, including potent activity against Aspergillus and Penicillium species.
    Echinoside A
  • 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-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-182748
    NL-26
    		Inhibitor
    NL-26 is a Topoisomerase I inhibitor. NL-26 stabilizes the covalent Topoisomerase I (Topo I)-DNA complex, prevents DNA religation and triggers the DNA damage response. NL-26 induces G2/M cell cycle arrest and apoptosis in cancer cells. NL-26 can be used for the research of colorectal cancer.
    NL-26
  • 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-W754608
    EIDD 1931-13C,15N2
    EIDD 1931-13C,15N2 (β-D-N4-Hydroxycytidine-13C,15N2) is the 13C- and 15N-labeled EIDD 19312 (HY-125033). EIDD-1931 (Beta-d-N4-hydroxycytidine; NHC) is a novel nucleoside analog and behaves as a potent?anti-virus agent. EIDD-1931 effectively inhibits the replication activity of?venezuelan equine encephalitis?virus (VEEV),?Chikungunya?virus (CHIKV) and?hepatitis?C virus (HCV)
    EIDD 1931-<sup>13</sup>C,<sup>15</sup>N<sub>2</sub>
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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