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-101647A
    Intoplicine dimesylate
    		Inhibitor 98.28%
    Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA.
    Intoplicine dimesylate
  • HY-10919
    C-1311
    		Inhibitor
    C-1311 shows to inhibit the catalytic activity of DNA topoisomerase II in vitro and in tumour cells. C-1311 prolongs G2 arrest followed by G2 to M transit and cell death during mitosis in the process of mitotic catastrophe.
    C-1311
  • HY-115991
    Topoisomerase IV inhibitor 2
    		Inhibitor
    Topoisomerase IV inhibitor 2 (compound 5d) is a potent DNA topoisomerase IV (TOPO IV) inhibitor with IC50s of 0.35 μM and 0.55 μM for TOPO IV and DNA gyrase, respectively. Topoisomerase IV inhibitor 2 has anti-bacterial activity, with MICs of 1.985 μM and 0.744 μM in Staphylococcus aureus Newman and Escherichia coli ATCC8739, respectively.
    Topoisomerase IV inhibitor 2
  • HY-158230
    SN-398
    		Inhibitor
    SN-398 is a derivative of Camptothecin (HY-158230), which is an antitumor drug. Acting by inhibiting mammalian DNA topoisomerase I (Topo I), stabilizing the Topo I-DNA complex prevents DNA rewiring to induce Topo I mediated DNA breaks. In Hela cell tests, SN-398 shows stronger antitumor activity than SN-38 (HY-13704) (IC50=1.562 μM). SN-398 can be used to study the anti-proliferation and growth inhibition of Topo I in cancer cells.
    SN-398
  • HY-146163
    Topoisomerase II inhibitor 7
    		Inhibitor
    Topoisomerase II inhibitor 7 (compound 3a) is a potent inhibitor of topoisomerase II alpha subtype, with an IC50 of 3.19 μM. Topoisomerase II inhibitor 7 can induce cell cycle arrest and apoptosis.
    Topoisomerase II inhibitor 7
  • HY-13551B
    Amsacrine (gluconate)
    		Inhibitor
    Amsacrine gluconate is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
    Amsacrine (gluconate)
  • HY-146497
    Topoisomerase I inhibitor 7
    		Inhibitor
    Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants. Topoisomerase I inhibitor 7 indicates prospects for further search of new antitumor agent candidates among the heteroarene-fused anthraquinones.
    Topoisomerase I inhibitor 7
  • HY-159483
    SelB-1
    		Inhibitor
    SelB-1 serves as a dual inhibitor for Topoisomerase I/II. SelB-1 possesses anticancer activity and can be utilized in the research of prostate cancer and colon cancer. Furthermore, SelB-1 is also capable of inducing autophagy gene expression and lipid peroxidation, while simultaneously reducing the level of GSH.
    SelB-1
  • 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-18258S
    Berberine-d6 chloride
    		Inhibitor
    Berberine-d6 (chloride) is the deuterium labeled Berberine chloride. Berberine chloride is an alkaloid that acts as an antibiotic. Berberine chloride induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties[1].
    Berberine-d<sub>6</sub> chloride
  • 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-N6621A
    Hippeastrine hydrobromide
    		Inhibitor
    Hippeastrine hydrobromide is an active alkaloid that exhibits a good dose-dependent inhibitory effect on topoisomerase I (Top I) with an IC50 of 7.25?μg/mL. Hippeastrine hydrobromide exhibits antiproliferative and anticancer activities.
    Hippeastrine hydrobromide
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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