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-147801
    Topoisomerase IIα-IN-3
    		Inhibitor
    Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cell cycle at the G0/G1 phase and induces apoptosis.
    Topoisomerase IIα-IN-3
  • HY-149002
    Topoisomerase I/II inhibitor 4
    		Inhibitor
    Topoisomerase I/II inhibitor 4 (compound F16) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 4 inhibits cell proliferation, invasion and migration and induces apoptosis. Topoisomerase I/II inhibitor 4 can be used for liver cancer research.
    Topoisomerase I/II inhibitor 4
  • HY-14871
    Tenifatecan
    		Inhibitor
    Tenifatecan (SN2310) is an injectable emulsion composed of vitamin E, a succinate derivative, as well as 7-ethyl-10-hydroxycamptothecin (SN-38, the active metabolite of irinotecan). Tenifatecan (SN2310) possesses anticancer activity.
    Tenifatecan
  • HY-168848
    KT32
    		Inhibitor
    KT32 (10c) is a potent dual inhibitor of HDAC and Topo II α. KT32 induces cell death through apoptosis.
    KT32
  • HY-17460AR
    Garenoxacin Mesylate hydrate (Standard)
    		Inhibitor
    ACHE-IN-38 (hydrochloride) (Standard) is the analytical standard of ACHE-IN-38 (hydrochloride). This product is intended for research and analytical applications. ACHE-IN-38 hydrochloride (Compound 13b) inhibits the metabolic breakdown of the neurotransmitter acetylcholine (ACh) by the enzyme acetylcholinesterase (AChE) and hence alleviates memory deficits in patients with Alzheimer’s Disease by potentiating cholinergic transmission.
    Garenoxacin Mesylate hydrate (Standard)
  • HY-B0330BR
    Levofloxacin hydrochloride (Standard)
    		Inhibitor
    Levofloxacin (hydrochloride) (Standard) is the analytical standard of Levofloxacin (hydrochloride). This product is intended for research and analytical applications. Levofloxacin ((-)-Ofloxacin) hydrochloride is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrochloride inhibits the DNA gyrase and topoisomerase IV. Levofloxacin hydrochloride can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin hydrochloride shows anti-orthopoxvirus activity[1][2][3][4][5].
    Levofloxacin hydrochloride (Standard)
  • HY-171138
    Mal-VC-PAB-DMEA-PNU-159682
    		Inhibitor
    Mal-VC-PAB-DMEA-PNU-159682 is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-topoisomerase II agent, PNU-159682, linked via the lysosomally cleavable dipeptide, Mc-VC-PAB. Mal-VC-PAB-DMEA-PNU-159682 can be used in the synthesis of Anti-CD22-NMS249 (HY-164761).
    Mal-VC-PAB-DMEA-PNU-159682
  • HY-105387
    Heliquinomycin
    		Inhibitor
    Heliquinomycin is an inhibitor of DNA helicase (Ki: 6.8 μM) and inhibits DNA and RNA synthesis. Heliquinomycin is effective against Gram-positive bacteria strains. Heliquinomycin inhibits cancer cell growth.
    Heliquinomycin
  • 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-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-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-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-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-113642
    CP-67804
    CP-67804 is a quinolone derivative, is a topoisomerase II-targeted agent. CP-67804 effectively enhances DNA cleavage mediated by eukaryotic topoisomerase II. CP-67804 has potential as an antineoplastic agent.
    CP-67804
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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