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-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-13704R
    SN-38 (Standard)
    		Inhibitor
    SN-38 (Standard) is the analytical standard of SN-38. This product is intended for research and analytical applications. SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254).
    SN-38 (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-13629R
    Etoposide (Standard)
    		Inhibitor
    Etoposide (Standard) is the analytical standard of Etoposide. This product is intended for research and analytical applications. Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy.
    Etoposide (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-W010800R
    Cholesteryl hemisuccinate (Standard)
    		Inhibitor
    Cholesteryl hemisuccinate (Standard) is the analytical standard of Cholesteryl hemisuccinate. This product is intended for research and analytical applications. Cholesteryl hemisuccinate is a with hepatoprotective an anticancer activity. Cholesteryl hemisuccinate inhibits Acetaminophen (AAP, HY-66005) hepatotoxicity, and prevents AAP-induced hepatic apoptosis and necrosis. Cholesteryl hemisuccinate inhibits DNA polymerase and DNA topoisomerase to inhibit DNA replication and repair and cell division. Thus, Cholesteryl hemisuccinate inhibits tumor growth[1][2].
    Cholesteryl hemisuccinate (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[1].
    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
  • HY-17460
    Garenoxacin
    		Inhibitor
    Garenoxacin (BMS284756) is an orally active quinolone antibiotic and has a broad spectrum of activity against a wide array of gram-positive and gram-negative bacteria, anaerobes, and fastidious organisms.
    Garenoxacin
  • HY-100875R
    Bisantrene (Standard)
    		Inhibitor
    Bisantrene (Standard) is the analytical standard of Bisantrene. This product is intended for research and analytical applications. Bisantrene is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene targets eukaryotic type II topoisomerases. Bisantrene is a substrate of MDR1[1][2][3][4].
    Bisantrene (Standard)
  • HY-170567
    DNA gyrase/Topo IV-IN-1
    		Inhibitor
    DNA gyrase/Topo IV-IN-1 (Compound 27) is an inhibitor of DNA gyrase and topoisomerase IV, exhibiting antibacterial activity. For Escherichia coli and methicillin-resistant Staphylococcus aureus DNA gyrases, DNA gyrase/Topo IV-IN-1 has an IC50 of 11 and 17 nM respectively, and for topoisomerase IV of Escherichia coli and methicillin-resistant Staphylococcus aureus, the IC50 values are 83 and 21 nM respectively. DNA gyrase/Topo IV-IN-1 can be used for research in the field of anti-infection.
    DNA gyrase/Topo IV-IN-1
  • HY-160543
    Exatecan-amide-CH2-O-CH2-CH2-OH
    		Inhibitor
    Exatecan-amide-CH2-O-CH2-CH2-OH (Compound 4) is a derivative of Exatecan (HY-13631). Exatecan-amide-CH2-O-CH2-CH2-OH can be used for the research of cell proliferative diseases such as cancer.
    Exatecan-amide-CH2-O-CH2-CH2-OH
  • HY-W654130
    Daunorubicin-13C,d3
    		Inhibitor
    Daunorubicin-13C,d3 is 13C and deuterium labeled Daunorubicin. Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
    Daunorubicin-<sup>13</sup>C,d<sub>3</sub>
  • HY-125580
    Makaluvamine A
    		Inhibitor
    Makaluvamine A is a member of Makaluvamines. Makaluvamines can be isolated from Fijian sponges of the genus Zyzzya, and possess inhibitory activity toward topoisomerase II along with cytotoxic activity against HCT-116 human colon cancer cells.
    Makaluvamine A
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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