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-13062AS
    Daunorubicin-13C,d3 TFA
    		Inhibitor
    Daunorubicin-13C,d3 TFA (Daunomycin-13C,d3 TFA) is the deuterium and 13C-labeled Daunorubicin TFA. Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
    Daunorubicin-<sup>13</sup>C,d<sub>3</sub> TFA
  • 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
  • HY-169299
    TOPOI/PARP-1-IN-2
    		Inhibitor
    TOPOI/PARP-1-IN-2 (compound 6c) is a dual PARP-1 and topoisomerase 1 (TOPO-1) inhibitor with IC50s of 32.2 nM and 46.2 nM, respectively. TOPOI/PARP-1-IN-2 shows a selectivity for PARP-1 over PARP-2. TOPOI/PARP-1-IN-2 disrupts the cell cycle at the S phase and induces apoptosis in NCI-60 cancer cell lines.
    TOPOI/PARP-1-IN-2
  • HY-150755
    Topo I/COX-2-IN-2
    		Inhibitor
    Topo I/COX-2-IN-2 (Compound W10) is a potent dual-target inhibitor of Topo I and COX-2 with IC50 values of 0.90 μM and 2.31 μM, respectively. Topo I/COX-2-IN-2 induces cancer cell apoptosis through the mitochondrial pathway.
    Topo I/COX-2-IN-2
  • HY-126333
    Topoisomerase II inhibitor 1
    		Inhibitor 99.9%
    Topoisomerase II inhibitor 1 (compound 89) is a highly efficient and selective topoisomerase IIα inhibitor.
    Topoisomerase II inhibitor 1
  • HY-B0147R
    Pefloxacin (Standard)
    Pefloxacin (Standard) (Pefloxacinium (Standard)) is the analytical standard of Pefloxacin (HY-B0147). This product is intended for research and analytical applications. Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies.
    Pefloxacin (Standard)
  • HY-107044
    DK 507k
    		Modulator
    DK 507k is an orally active 8-methoxyquinolone Antibacterial agent. DK 507k targets DNA gyrase subunit A (GyrA) and modulates the function of GyrA. DK 507k inhibits the growth of various Gram-positive and Gram-negative bacteria, including Pseudomonas aeruginosa and Methicillin (HY-121544)-resistant Staphylococcus aureus. DK 507k eliminates Penicillin-tolerant Streptococcus pneumoniae from the lungs of mice. DK 507k can be used in research related to sepsis and *Streptococcus pneumoniae* pneumonia.
    DK 507k
  • HY-E70899
    Topoisomerase IV, Streptococcus pneumoniae
    Topoisomerase IV, Streptococcus pneumoniae (EC 5.99.1.) is prepared by overexpressing the subunits in E. coli.
    Topoisomerase IV, Streptococcus pneumoniae
  • HY-147861
    Topoisomerase II inhibitor 11
    		Inhibitor
    Topoisomerase II inhibitor 11 (compound 3d) is a potent Topoisomerase II inhibitor, with an IC50 of 2.89 μM. Topoisomerase II inhibitor 11 shows 92.46% inhibition on renal cancer cell line A498 with an IC50 of 3.5 μM. Topoisomerase II inhibitor 11 causes cell cycle arrest at the G2/M phase leading to cell proliferation inhibition and pro-apoptotic activity.
    Topoisomerase II inhibitor 11
  • HY-119827
    Moflomycin
    		Agonist
    Moflomycin (F 860191) is a compound with strong anti-leukemic activity and low mutagenicity. Moflomycin has an antiproliferative effect on the leukemic cell line HL60 in vitro (IC50=2.9 nM). Moflomycin enhances topoisomerase II-induced DNA breaks and free radical production.
    Moflomycin
  • HY-137005
    CS1
    		Inhibitor
    CS1 is a potent DNA Topo II α inhibitor. CS1 displays broad-spectrum in vitro antitumor effects, low toxicity in vivo and potential anti-multidrug resistance capabilities. CS1 leads to DNA damage, cell cycle arrest at G2/M phase and apoptosis.
    CS1
  • HY-178145
    Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan
    		Inhibitor
    Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan (compound 12) is a Drug-Linker Conjugate for ADC. Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan contains the ADC linker (Mc-Lys(PEG12)-Cap-Ala-Ala-PABC) (HY-178146) and a DNA topoisomerase I inhibitor Exatecan (HY-13631). Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan can be used for the development of ADC targeting HER2-positive breast cancer.
    Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan
  • HY-13631T
    (1R,9S)-Exatecan
    (1R,9S)-Exatecan (DX8951f) is the (1R,9S) stereoisomer of Exatecan (HY-13631). Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
    (1R,9S)-Exatecan
  • HY-N2331R
    Proscillaridin A (Standard)
    		Inhibitor
    Proscillaridin A (Standard) is the analytical standard of Proscillaridin A. This product is intended for research and analytical applications. Proscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively.
    Proscillaridin A (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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