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-119458
    Luotonin A
    		Inhibitor
    Luotonin A is an antiviral and antiphytopathogenic fungus agent. Luotonin A has good antiviral activity against tobacco mosaic virus (TMV). Luotonin A also has certain inhibitory activity on topoisomerase I and topoisomerase II. Luotonin A shows antitumor activity.
    Luotonin A
  • HY-13502S
    Mitoxantrone-d8
    		Inhibitor
    Mitoxantrone-d8 (mitozantrone-d8) is the deuterium labeled Mitoxantrone. Mitoxantrone is a topoisomerase II inhibitor and also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM[1][2].
    Mitoxantrone-d<sub>8</sub>
  • HY-10581AS
    Gatifloxacin-d3 hydrochloride
    		Inhibitor
    Gatifloxacin-d3 (hydrochloride) is the deuterium labeled Gatifloxacin (hydrochloride). Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
    Gatifloxacin-d<sub>3</sub> hydrochloride
  • HY-124552
    Epolactaene
    		Inhibitor
    Epolactaene is a potent Topoisomerase II and DNA Polymerase inhibitor with IC50 values of 10, 25, 94 µM for Topoisomerase II, DNA Polymerase α, DNA Polymerase β, respectively.
    Epolactaene
  • HY-143266
    Topoisomerase I inhibitor 3
    		Inhibitor
    Topoisomerase I inhibitor 3 (Compound ZML-14) is a topoisomerase I inhibitor and can interact with topoisomerase I-DNA complex. Topoisomerase I inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2/M phase.
    Topoisomerase I inhibitor 3
  • HY-146816
    NBTIs-IN-6
    		Inhibitor
    NBTIs-IN-6 is a bacterial topoisomerase inhibitor with certain antibacterial activity. Among them, the MIC90 for fluoroquinolone-resistant MRSA was 2 μg/mL.
    NBTIs-IN-6
  • HY-147877
    Topoisomerase II inhibitor 12
    		Inhibitor
    Topoisomerase II inhibitor 12 (Compound 8c) is a topoisomerase II (topo II) inhibitor, working as a DNA non-intercalator. Topoisomerase II inhibitor 12 shows antineoplastic activity.
    Topoisomerase II inhibitor 12
  • HY-162381
    Topoisomerase II inhibitor 19
    		Inhibitor
    Topoisomerase II inhibitor 19 (compound 5h) is a DNA intercalator and topoisomerase II inhibitor (IC50 value of 0.34 μM). Topoisomerase II inhibitor 19 would induce detectable potent damage in ctDNA.
    Topoisomerase II inhibitor 19
  • HY-B0526S
    Flumequine-13C3
    		Inhibitor
    Flumequine-13C3 is the 13C3 labeled Flumequine. 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-<sup>13</sup>C<sub>3</sub>
  • HY-149410
    MSN8C
    		Inhibitor
    MSN8C, an analog of mansonone E, is a novel catalytic inhibitor of human DNA topoisomerase II. MSN8C induces cancer cell apoptosis. MSN8C shows significant anti-tumor cell proliferation activity in vitro.
    MSN8C
  • HY-N10367
    Corydamine
    		Inhibitor
    Corydamine, 3-arylisoquinoline alkaloid, is a potent DNA topoisomerase I/II inhibitor. Corydamine has anti-cancer activity.
    Corydamine
  • HY-143301
    Topoisomerase I inhibitor 4
    		Inhibitor
    Topoisomerase I inhibitor 4 (compound 7a) is a topoisomerase I inhibitor. Topoisomerase I inhibitor 4 inhibits HepG2, A549, MCF-7 and HeLa cancer cells proliferation with IC50s of 1.20, 2.09, 1.56 and 1.92 μM, respectively. Topoisomerase I inhibitor 4 can be used for the research of cancer.
    Topoisomerase I inhibitor 4
  • HY-150045
    TP0480066
    		Inhibitor
    TP0480066 is a selective topoisomerase II inhibitor with IC50s of 1.10 and 62.89 nM for DNA gyrase and topo IV, respectively. TP0480066 shows good activity of againsting various bacterial species including drug-resistant strains. TP0480066 also exhibits potent inhibitory activity to N. gonorrhoeae, can be used in study of gonorrhea.
    TP0480066
  • HY-12888
    AZD5099
    		Inhibitor
    AZD5099, an antibacterial agent, is a potent and selective bacterial topoisomerase II inhibitor. AZD5099 potently inhibits the infections caused by Gram-positive and fastidious Gram-negative bacteria.
    AZD5099
  • HY-N8473
    Pericosine A
    		Inhibitor
    Pericosine A ((+)-Pericosine A) is a topoisomerase II (Topoisomerase II) inhibitor that can be isolated from the Periconia byssoides strain. Pericosine A has significant antitumor activity in vitro and in vivo and can be used in cancer research. Pericosine A also inhibits the protein kinase epidermal growth factor receptor.
    Pericosine A
  • HY-153069A
    GGFG-PAB-Exatecan TFA
    		Inhibitor
    GGFG-PAB-Exatecan TFA consists of an ADC toxin Exatecan (HY-13631) and a linker GGFG-PAB, and can be used as a drug-linker conjugate for the synthesis of ADC molecules.
    GGFG-PAB-Exatecan TFA
  • HY-79490S
    Ac-Exatecan-d5
    		Inhibitor 99.93%
    Ac-Exatecan-d5 is the deuterium labeled Ac-Exatecan (HY-79490).
    Ac-Exatecan-d<sub>5</sub>
  • HY-161385
    Topoisomerase I inhibitor 16
    		Inhibitor
    Topoisomerase I inhibitor 21 (Compound 3e) is an inhibitor for Topoisomerase I through stabilization of enzyme-DNA complex. Topoisomerase I inhibitor 21 exhibits antiproliferative activity in 39 human cancer cells (JFCR39) with mean GI50 39 nM.
    Topoisomerase I inhibitor 16
  • HY-N6714R
    Alternariol (Standard)
    		Inhibitor
    Alternariol (Standard) is the analytical standard of Alternariol. This product is intended for research and analytical applications. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects.
    Alternariol (Standard)
  • HY-135845
    TP3011
    		Inhibitor
    TP3011 (CH0793011) is an active metabolite of CH-0793076 and is a potent topoisomerase I inhibitor equipotent as SN38. TP3011 is against cancer cell lines growth with IC50s at the range sub-nanomolar in vitro.
    TP3011
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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