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-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-179520
    XSJ151
    		Inhibitor
    XSJ151 is a topoisomerase I inhibitor, stabilizing the DNA-Topo I covalent complex and inducing DNA double-strand breaks. XSJ151-induces DNA damage activates the p53-p21 signaling pathway, specifically regulating the expression of cyclins, leading to G2/M phase cell cycle arrest and disrupting the dynamic homeostasis of Bcl-2 family proteins, thereby triggering apoptosis in gastric cancer cells. XSJ151 can be used for the study of gastric cancer.
    XSJ151
  • 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-175853
    Topoisomerase II-IN-24
    		Inhibitor
    Topoisomerase II-IN-24 is a Topoisomerase IIα inhibitor with an IC50 of 41.67 μM. Topoisomerase II-IN-24 can inhibit cancer cells proliferation, induce G2/M phase arrest and induce apoptosis. Topoisomerase II-IN-24 can be used for the research of cancer, such as colon cancer.
    Topoisomerase II-IN-24
  • HY-N19832
    Icariside E3
    		Inhibitor
    Icariside E3 is a Leishmania donovani DNA Topoisomerase IB (LdTOP1LS) inhibitor. Icariside E3 can be used for the research of leishmaniasis.
    Icariside E3
  • 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-180508
    MDM2-IN-27
    		Inhibitor
    MDM2-IN-27 (Compound 20k) is an MDM2 inhibitor. MDM2-IN-27 can effectively block the inhibitory effect of MDM2 on p53, thereby activating the p53 pathway. MDM2-IN-27 has a certain topoisomerase I inhibitory activity and has a very weak inhibitory effect on topoisomerase IIα. MDM2-IN-27 exhibits significant anti-proliferative activity against breast cancer, colon cancer, and cutaneous squamous cell carcinoma.
    MDM2-IN-27
  • HY-178174
    MGB4
    		Inhibitor
    MGB4 is a DNA minor groove binder. MGB4 binds to ARE-containing DNA and inhibition of topoisomerase I activity. MGB4 can impacts key cellular pathways, including inhibition oftranslation and alterations in sphingolipid and amino acid metabolism. MGB4 also reduces spermine and spermidine metabolism companied with Doxorubicin (HY-15142A). MGB4 can be used for the research of cancer, such as Prostate cancer.
    MGB4
  • 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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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