1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. Topoisomerase

Topoisomerase

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-19943
    TLC388
    Inhibitor
    TLC388 is a novel camptothecin analog with limited antitumor activity in metastatic NEC.
    TLC388
  • HY-145290
    CPT-Se3
    Inhibitor
    CPT-Se3, a selenoproagent of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT–Se3 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se3 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC50= 2.19-4.7 μM).
    CPT-Se3
  • HY-169628
    Topoisomerase I/II inhibitor 7
    Inhibitor
    Topoisomerase I/II inhibitor 7 (Compound 5h) is a Topoisomerase I/II inhibitor.
    Topoisomerase I/II inhibitor 7
  • HY-158138
    TOPOI/PARP-1-IN-1
    Inhibitor
    TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4%.
    TOPOI/PARP-1-IN-1
  • HY-W338859
    Levofloxacin mesylate
    Inhibitor
    Levofloxacin mesylate is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin mesylate inhibits the DNA gyrase and topoisomerase IV. Levofloxacin mesylate can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin mesylate shows anti-orthopoxvirus activity.
    Levofloxacin mesylate
  • HY-152479
    Topoisomerase IIα-IN-7
    Inhibitor
    Topoisomerase IIα-IN-7 is an DNA topoisomerase IIα inhibitor with an IC50 value of 7.7 µM. Topoisomerase IIα-IN-7 has broad-spectrum cytotoxicity to leukemia, lung, colon, melanoma, ovarian, kidney, prostate and breast cancer cells. Topoisomerase IIα-IN-7 has metabolic stability.
    Topoisomerase IIα-IN-7
  • HY-18351A
    Indotecan hydrochloride
    Inhibitor
    Indotecan hydrochloride, an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan hydrochloride prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis.
    Indotecan hydrochloride
  • HY-114983
    Chimmitecan
    Inhibitor 98.96%
    Chimmitecan ((S)-9-Allyl-10-Hydroxycamptothecin), a novel 9-small-alkyl-substituted lipophilic Camptothecin (HY-16560), is a potent inhibitor of topoisomerase I. Chimmitecan exhibits anticancer activity.
    Chimmitecan
  • HY-N6054
    Niranthin
    Inhibitor
    Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
    Niranthin
  • HY-B0067B
    (R)-Amrubicin
    Inhibitor
    (R)-Amrubicin ((R)-SM-5887) is an anthracycline that effectively treats lung cancer by intercalating into DNA and inhibiting topoisomerase II activity, which consequently hampers DNA replication as well as RNA and protein synthesis, leading to cell growth inhibition and apoptosis. This compound exhibits superior anti-tumor efficacy compared to traditional anthracycline drugs while lacking the cumulative cardiac toxicity typically associated with this drug class.
    (R)-Amrubicin
  • 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.
    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-173478
    OSUAB-0284
    Inhibitor
    OSUAB-0284 is a bacterial topoisomerase inhibitor. OSUAB-0284 has significant anti-staphylococcal activity, especially against methicillin-resistant Staphylococcus aureus (MRSA). OSUAB-0284 exerts its antibacterial effect by inhibiting bacterial topoisomerase. OSUAB-0284 can be used to study infections caused by drug-resistant bacteria such as MRSA.
    OSUAB-0284
  • 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>
Cat. No. Product Name / Synonyms Species Source
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