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-122481
    Thaspine acetate
    		Inhibitor
    Thaspine acetate, an alkaloid, is a topoisomerase I and II inhibitor. Thaspine acetate induces cancer cell apoptosis. Thaspine acetate induces Bak and Bax activation, mitochondrial cytochrome c release and mitochondrial membrane permeabilization. Thaspine acetate can be isoalted from the cortex of the South American tree Croton lechleri.
    Thaspine acetate
  • HY-400316
    Exatecan intermediate 8
    		Inhibitor
    Exatecan intermediate 8 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 8
  • HY-13566R
    Belotecan (Standard)
    		Inhibitor
    Belotecan (Standard) is the analytical standard of Belotecan. This product is intended for research and analytical applications. Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer.
    Belotecan (Standard)
  • HY-161813
    Antibacterial agent 229
    		Inhibitor
    Antibacterial agent 229 (compound 8a) is a potent antibacterial agent. Antibacterial agent 229 shows antibacterial and antifungal abilities. Antibacterial agent 229 disrupts the integrity of the bacterial membrane, intercalates into DNA. Antibacterial agent 229 inhibits topoisomerase IV with an IC50 value of 10.88 µM.
    Antibacterial agent 229
  • HY-117657
    (-)-BO 2367
    		Inhibitor
    (-)-BO 2367, an antimicrobial quinolone, is a strong mammalian and bacterial topoisomerase II inhibitor. (-)-BO 2367 shows IC50 values with 3.8 μM, 0.5 μM, and 1 μM against the DNA relaxation activity of L1210 topoisomerase II and the supercoiling activities of Escherichia coli gyrase and Micrococcus luteus gyrase, respectively. (-)-BO 2367 is a potent antitumor agent.
    (-)-BO 2367
  • HY-16562R
    Irinotecan (Standard)
    		Inhibitor
    Irinotecan (Standard) is the analytical standard of Irinotecan. This product is intended for research and analytical applications. Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
    Irinotecan (Standard)
  • HY-W178011
    Topoisomerase IIα-IN-9
    		Inhibitor
    Topoisomerase IIα-IN-9 (NSC85582) is a bisphenol compound that has a moderate inhibitory effect on DNA topoisomerase Topoisomerase II (IC50: 571 μM). Topoisomerase IIα-IN-9 also exhibits a certain cell growth inhibitory effect, with IC50s of 117 μM and 218 μM for K562 and CHO, respectively.
    Topoisomerase IIα-IN-9
  • HY-B0879AR
    Suramin sodium salt (Standard)
    		Inhibitor
    Suramin (sodium salt) (Standard) is the analytical standard of Suramin (sodium salt). This product is intended for research and analytical applications. Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor. Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
    Suramin sodium salt (Standard)
  • HY-13551R
    Amsacrine (Standard)
    		Inhibitor
    Amsacrine (Standard) is the analytical standard of Amsacrine. This product is intended for research and analytical applications. Amsacrine (m-AMSA; acridinyl anisidide) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
    Amsacrine (Standard)
  • HY-106702A
    Fostriecin
    		Inhibitor
    Fostriecin is a triene antibiotic. Fostriecin is a topoisomerase II and protein phosphatase PP2A inhibitor.
    Fostriecin
  • HY-13565
    Becatecarin
    		Inhibitor
    Becatecarin is a rebeccamycin analog with antitumor effects. Becatecarin intercalates into DNA and inhibites the catalytic activity of topoisomerases I/II.
    Becatecarin
  • HY-134290A
    8-Chloro-ATP tetrasodium
    		Inhibitor
    8-Chloro-ATP tetrasodium, an ATP (HY-B2176) analog, is a topoisomerase II (Topo II) inhibitor. 8-Chloro-ATP tetrasodium inhibits DNA synthesis and induces DNA double-stranded breaks (DSBs). 8-Chloro-ATP tetrasodium inhibits Topo II-catalyzed ATP hydrolysis.
    8-Chloro-ATP tetrasodium
  • HY-161937
    Antibacterial agent 236
    		Inhibitor
    Antibacterial agent 236 (Compound 4l) is an orally active inhibitor for DNA gyrase and topoisomerase IV (IC50 is 3.2 and 300 nM in Staphylococcus aureus), and exhibits board-spectrum antibacterial activity. Antibacterial agent 236 exhibits good pharmacokinetic properties in mice.
    Antibacterial agent 236
  • HY-B0398S
    Nalidixic Acid-d5
    		Inhibitor
    Nalidixic Acid-d5 is the deuterium labeled Nalidixic acid. Nalidixic acid, a quinolone antibiotic, is effective against both gram-positive and gram-negative bacteria. Nalidixic acid acts in a bacteriostatic manner in lower concentrations and is bactericidal in higher concentrations. Nalidixic acid inhibits a subunit of DNA gyrase and topoisomerase IV and reversibly blocks DNA replication in susceptible bacteria.
    Nalidixic Acid-d<sub>5</sub>
  • HY-13562AR
    Banoxantrone dihydrochloride (Standard)
    		Inhibitor
    Banoxantrone (dihydrochloride) (Standard) is the analytical standard of Banoxantrone (dihydrochloride). This product is intended for research and analytical applications. Banoxantrone dihydrochloride is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
    Banoxantrone dihydrochloride (Standard)
  • HY-13768AR
    Topotecan hydrochloride (Standard)
    		Inhibitor
    Topotecan (hydrochloride) (Standard) is the analytical standard of Topotecan (hydrochloride). This product is intended for research and analytical applications. Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.
    Topotecan hydrochloride (Standard)
  • HY-13629S
    Etoposide-d3
    		Inhibitor
    Etoposide-d3 (VP-16-d3) is the deuterium labeled Etoposide (HY-13629). Etoposide (VP-16) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy.
    Etoposide-d<sub>3</sub>
  • HY-100777R
    DACA (Standard)
    		Inhibitor
    DACA (Standard) is the analytical standard of DACA. This product is intended for research and analytical applications. DACA inhibits two essential nuclear enzymes in vitro, DNA topoisomerase I and DNA topoisomerase (topo) II. DACA stabilises topo I, topo II alpha, and topo II beta cleavable complexes in human leukaemia CCRF-CEM cells.
    DACA (Standard)
  • HY-13761R
    Teniposide (Standard)
    		Inhibitor
    Teniposide (Standard) is the analytical standard of Teniposide. This product is intended for research and analytical applications. Teniposide is a podophyllotoxin derivative, acts as a topoisomerase II inhibitor, and used as a chemotherapeutic agent.
    Teniposide (Standard)
  • HY-116231
    (S)-Gyramide A
    		Inhibitor
    (S)-Gyramide A is a weak inhibitor of cell proliferation that can target DNA gyrase.
    (S)-Gyramide A
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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