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-N1457
    Chrysosplenetin
    		Inhibitor 99.84%
    Chrysosplenetin is an orally active polymethoxyflavone. Chrysosplenetin exerts anticancer effects by inhibiting topoisomerase, protecting DNA and inducing apoptosis. Chrysosplenetin acts as an antimalarial sensitizer, reverses Artemisinin (HY-B0094) resistance by inhibiting and downregulating P-glycoprotein, and enhances the efficacy of Artemisinin. Chrysosplenetin promotes bone formation by activating the Wnt/β-catenin pathway and exerts anti-osteoporotic effects.
    Chrysosplenetin
  • HY-147408
    Rezetecan
    		Inhibitor 99.60%
    Rezetecan (SHR9265) is a topoisomerase I inhibitor. In addition, Rezetecan can be used to synthesize Trastuzumab rezetecan, an antineoplastic agent. Rezetecán can be used as a cytotoxic payload (ADC Cytotoxin) in antibody-drug conjugates (ADCs).
    Rezetecan
  • HY-14821
    Namitecan
    		Inhibitor 98.03%
    Namitecan is a potent topoisomerase I inhibitor, with antitumor property.
    Namitecan
  • HY-148380A
    Mal-PEG8-Phe-Lys-PAB-Exatecan TFA
    		Inhibitor 98.66%
    Mal-PEG8-Phe-Lys-PAB-Exatecan TFA is a agent-linker conjugate for ADC, composed of degradable linker Mal-PEG8-Phe-Lys-PAB and toxin molecule Exatecan (HY-13631).
    Mal-PEG8-Phe-Lys-PAB-Exatecan TFA
  • HY-N5038
    Mauritianin
    		Inhibitor 99.83%
    Mauritianin is an orally active kaempferol glycoside. Mauritianin can be isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor. Mauritianin has hepatoprotective, neuroprotective, and renoprotective activities. Mauritianin increases vascular tone when used in combination with Alcesefoliside (HY-N5049).
    Mauritianin
  • HY-N0114A
    (±)-Evodiamine
    		Inhibitor 99.74%
    (±)-Evodiamine, a quinazolinocarboline alkaloid, is a Top1 inhibitor. Evodiamine exhibits anti-inflammatory, antiobesity, and antitumor effects. (±)-Evodiamine inhibits the proliferation of a wide variety of tumor cells by inducing their apoptosis.
    (±)-Evodiamine
  • HY-175203
    Topi MF-6
    		Inhibitor 99.79%
    Topi MF-6 is a DNA topoisomerase I (Top1) inhibitor. Topi MF-6 can be used as an ADC payload.
    Topi MF-6
  • HY-158329
    Alloc-DOX
    		Inhibitor 98.40%
    Alloc-DOX (N-Alloc doxorubicin) is a Doxorubicin (HY-15142A) prodrug. The combination of a catalyst (such as nano-palladium) and alloc-DOX leads to a decrease in cell viability and tumour growth.
    Alloc-DOX
  • HY-122594
    BNS-22
    		Inhibitor 99.50%
    BNS-22 is a DNA topoisomerase II (TOP2) catalytic inhibitor with the IC50 values of 2.8 μM and 0.42 μM for human TOP2α and TOP2β, respectively. BNS-22 induces abnormal division and has anti-proliferative activity.
    BNS-22
  • HY-N10495
    Seconeolitsine
    		Inhibitor 98.65%
    Seconeolitsine, an antibiotic, and is an inhibitor of targeting topoisomerase I (TopA). Seconeolitsine also is a new antimicrobial agent that can inhibit S. pneumoniae growth. Seconeolitsine can inhibit TopA relaxation activity with an IC50 value of 17 μM. Seconeolitsine can be used for the research of S. pneumoniae infections resistant to other antibiotics.
    Seconeolitsine
  • HY-N0872
    Isosteviol
    		Inhibitor 99.86%
    Isosteviol ((-)-Isosteviol) is a derivative of Stevioside through acid catalyzed hydrolysis of Stevioside. Isosteviol inhibits DNA polymerase and DNA topoisomerase and has antibacterial, anticancer and anti-tuberculosis effects.
    Isosteviol
  • HY-43565
    Exatecan intermediate 9
    		Inhibitor 99.80%
    Exatecan intermediate 9 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM).
    Exatecan intermediate 9
  • HY-B0356AS1
    Ciprofloxacin-13C3,15N monohydrochloride
    		Inhibitor 99.9%
    Ciprofloxacin-13C3,15N (Bay-09867-13C3,15N) monohydrochloride is 13C- and 15N-labeled Ciprofloxacin (monohydrochloride) (HY-B0356A).
    Ciprofloxacin-<sup>13</sup>C<sub>3</sub>,<sup>15</sup>N monohydrochloride
  • HY-128995AS
    Glycyl-Exatecan-d5 hydrochloride
    		Inhibitor 98.97%
    Glycyl-Exatecan-d5 (Glycyl-DX-8951-d5) hydrochloride is deuterium labeled Glycyl-Exatecan (HY-128995A). Glycyl-Exatecan (Glycyl-DX-8951), a derivative of Exatecan (HY-13631), is an anticancer agent. Glycyl-Exatecan has significantly antitumor activity. Glycyl-Exatecan can be used for cancers like solid tumors research.
    Glycyl-Exatecan-d<sub>5</sub> hydrochloride
  • HY-148058
    Topoisomerase I inhibitor 8
    		Inhibitor 99.87%
    Topoisomerase I inhibitor 8 is a potent topoisomerase I inhibitor. Topoisomerase I inhibitor 8 is a hexacyclic analogue of camptothecin, and displays cytotoxic effect against tumor cells.
    Topoisomerase I inhibitor 8
  • HY-177546
    DBCO-PEG3-GGFG-Exatecan
    		Inhibitor
    DBCO-PEG3-GGFG-Exatecan is a Drug-linker conjugate for ADC. DBCO-PEG3-GGFG-Exatecan contains the ADC linker (DBCO-PEG3-GGFG) and a DNA topoisomerase I inhibitor Exatecan (HY-13631).
    DBCO-PEG3-GGFG-Exatecan
  • HY-14812
    Karenitecin
    		Inhibitor 98.02%
    Karenitecin (Cositecan) is a topoisomerase I inhibitor, with potent anti-cancer activity.
    Karenitecin
  • HY-153401
    Topoisomerase II inhibitor 13
    		Inhibitor 98.07%
    Topoisomerase II inhibitor 13 is a topoisomerase II (Topo II) inhibitor. Topoisomerase II inhibitor 13 shows antiproliferative activity against several cancer cells. Topoisomerase II inhibitor 13 induces cancer cells apoptosis.
    Topoisomerase II inhibitor 13
  • HY-153600
    GGFG-amide-glycol-amide-Exatecan
    		Inhibitor
    GGFG-amide-glycol-amide-Exatecan (Intermediate 2) is an Exatecan (HY-13631) derivative and can be used in the synthesis of antibody-drug conjugates (ADCs).
    GGFG-amide-glycol-amide-Exatecan
  • HY-106410A
    Zabofloxacin hydrochloride
    		Inhibitor 99.54%
    Zabofloxacin hydrochloride (DW-224a) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin hydrochloride has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia. Zabofloxacin hydrochloride is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP).
    Zabofloxacin hydrochloride
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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