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-178315
    Exatecan analog 38
    		Inhibitor
    Exatecan analog 38 is a camptothecin derivative with potent topoisomerase I inhibitory activity. Exatecan analog 38 can be connected to monoclonal antibodies via linkers to form antibody-drug conjugate (ADC) molecules. Exatecan analog 38 can be used for cancer research.
    Exatecan analog 38
  • HY-157402
    Topoisomerase II/EGFR-IN-1
    Topoisomerase II/EGFR-IN-1 is topoisomerase II/EGFR dual inhibitor. Topoisomerase II/EGFR-IN-1 has superior cytotoxic activity to MCF-7, A549 and HCT-116 cell lines, displays strong apoptotic activity and can be used for the research of cancer.
    Topoisomerase II/EGFR-IN-1
  • HY-106031A
    F-14512 hydrochloride
    		Inhibitor
    F-14512 hydrochloride is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 hydrochloride enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 hydrochloride exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 hydrochloride demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 hydrochloride could be used to study breast cancer.
    F-14512 hydrochloride
  • HY-177684
    N-(endo-BCN-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan)
    N-(endo-BCN-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-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-(endo-BCN-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
    N-(endo-BCN-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan)
  • HY-119228
    SN-28049
    SN-28049 is a new DNA-binding topoisomerase II-directed antitumor agent. SN-28049 activates the p53 pathway. SN-28049 exhibits anticancer activity against colorectal cancer.
    SN-28049
  • HY-175216
    Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6
    		Inhibitor
    Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6 is a drug-linker conjugate for ADC. Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6 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). Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6 can be used for synthesis of ADCs.
    Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6
  • HY-148696A
    Gly-Cyclopropane-Exatecan
    		Inhibitor
    Gly-Cyclopropane-Exatecan involves in the synthesis of anti-B7-H4 ADC, containing Exatecan (HY-13631), a DNA Topoisomerase I inhibitor. Gly-Cyclopropane-Exatecan participated in the formation of the ADC hu2F7-Exatecan (compound 34), which showed antitumor activity in vivo and in vitro.
    Gly-Cyclopropane-Exatecan
  • HY-W780694
    PD 124816
    		Inhibitor
    PD 124816 is an orally active fluoroquinolone antibiotic. PD 124816 exerts broad-spectrum antibacterial effects by inhibiting DNA gyrase (topoisomerase IV), and it has no cross-resistance with commonly used antibiotics. PD 124816 is effective against both Gram-positive and Gram-negative bacteria (MIC₉₀ ≤ 0.06 μg/mL), and the MIC₉₀ for anaerobic bacteria (Peptostreptococcus fragi) is 1 μg/mL. PD 124816 exhibits complete bactericidal activity in a mouse model of Mycobacterium leprae infection. PD 124816 can be used for studying mixed infections and infections caused by drug-resistant bacteria.
    PD 124816
  • HY-122014
    S 39625
    		Inhibitor
    39625 is a camptothecin ketone analogue, a stable, potent and selective topoisomerase I inhibitor, active against purified topoisomerase I and cytotoxic to cancer cells.
    S 39625
  • HY-174151
    XSJ110
    		Inhibitor
    XSJ110 is a potent irreversible topoisomerase I (Topo I) inhibitor with an IC50 value of 0.133 μM. XSJ110 blocks DNA topoisomerization, induces DNA double-strand breaks, and triggers cell cycle arrest at G0/G1 phase, inducing tumor cell apoptosis. XSJ110 is promising for research of ampullary carcinoma (AC).
    XSJ110
  • HY-120173
    Ro 47-3359
    Ro 47-3359 is a pyrimido[1,6-a]benzimidazole compound with the activity of enhancing eukaryotic topoisomerase II-mediated DNA cleavage and being toxic to Kc cells.
    Ro 47-3359
  • HY-155645
    Topoisomerase II inhibitor 15
    		Inhibitor
    Topoisomerase II inhibitor 15 (compound 2g) is a Topoisomerase II inhibitor. Topoisomerase II inhibitor 15 potently is an apoptotic inducer with greater selectivity against head and neck tumors.
    Topoisomerase II inhibitor 15
  • HY-145397A
    (R)-(4-NH2)-Exatecan
    		Inhibitor
    (R)-(4-NH2)-Exatecan is the R enantiomer of (4-NH2)-Exatecan (Compound A). (R)-(4-NH2)-Exatecan, a topoisomerase inhibitor, is a derivative of Exatecan. (R)-(4-NH2)-Exatecan can be used in the synthesis of antibody-drug conjugates (ADCs).
    (R)-(4-NH2)-Exatecan
  • HY-164380
    MC-Val-Cit-Gly-exatecan-β-D-glucopyranosiduronic acid
    		Ligand
    MC-Val-Cit-Gly-exatecan-β-D-glucopyranosiduronic acid (example 13) is a drug-linker conjugate that consists of a DNA topoisomerase I inhibitor Exatecan (HY-13631) and a linker (HY-180841). MC-Val-Cit-Gly-exatecan-β-D-glucopyranosiduronic acid can be used in synthesis of ADC.
    MC-Val-Cit-Gly-exatecan-β-D-glucopyranosiduronic acid
  • HY-156723
    9-Chloromethyl-10-hydroxy-11-F-Camptothecin
    9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a novel camptothecin derivatives. 9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a DNA topoisomerase I (Topo I) inhibitor, can be used in anticancer research.
    9-Chloromethyl-10-hydroxy-11-F-Camptothecin
  • HY-180414
    Premafloxacin
    		Inhibitor
    Premafloxacin is a potent antimicrobial agent that exhibits activity against Staphylococcus aureus, Corynebacterium bovis, and Corynebacterium amylocolatum. Premafloxacin demonstrated potent antimicrobial activity against S. aureus by targeting topoisomerase IV, and is a poor substrate for NorA efflux pump. Premafloxacin can be used for antimicrobial research.
    Premafloxacin
  • HY-147971
    Anticancer agent 75
    		Inhibitor
    Anticancer agent 75 is a potent anticancer agent. Anticancer agent 75 shows cytotoxicity and selectivity in cancer cell lines. Anticancer agent 75 shows cytotoxicity to normal human kidney cell lines is at least 35 times lower than that of the Doxorubicin standard. Anticancer agent 75 shows good activity of antiplasmodial.
    Anticancer agent 75
  • HY-W713570
    Nectandrin B
    		Inhibitor
    Nectandrin B is an inhibitor of DNA topoisomerases I and II, which is found in Saururus chinensis. Nectandrin B is promising for research of cancers.
    Nectandrin B
  • HY-106556
    Zorubicin
    Zorubicin (Rubidazon) is a derivative of Daunorubicin (HY-13062A). Zorubicin interacts with topoisomerase II and inhibits DNA polymerases. Zorubicin can be used for the research of acute leukemias and sarcomas.
    Zorubicin
  • HY-111047
    GSK945237
    		Inhibitor
    GSK945237 is a potent and orally active bacterial type IIA topoisomerases inhibitor. GSK945237 shows broad-spectrum activity against Gram-positive and Gram-negative bacteria (IC50 of 0.034 μg/mL against H. influenzae DNA gyrase). GSK945237 demonstrates good in vivo efficacy in a rat respiratory tract infection model. GSK945237 can be used for anti-infection research.
    GSK945237
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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