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-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-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.
    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.
    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-B0395E
    (1S,2R,7S)-Sitafloxacin
    		Inhibitor
    (1S,2R,7S)-Sitafloxacin (DU-6856) is an enantiomer of Sitafloxacin (HY-B0395). (1S,2R,7S)-Sitafloxacin is a topoisomerase inhibitor. (1S,2R,7S)-Sitafloxacin is an antibiotic. (1S,2R,7S)-Sitafloxacin has inhibitory activity against Escherichia coli DNA gyrase (IC50 0.18 μg/mL) and Staphylococcus aureus topoisomerase IV. (1S,2R,7S)-Sitafloxacin has antibacterial activity and can be used in the study of various bacterial infections.
    (1S,2R,7S)-Sitafloxacin
  • HY-173458
    NBTIs-IN-7
    		Inhibitor
    NBTIs-IN-7 (compound 276) is a novel bacterial topoisomerase (NBTIs) inhibitor. NBTIs-IN-7 induces both single- and double-strand DNA strand breaks in the presence of gyrase.
    NBTIs-IN-7
  • 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
  • HY-13502AS1
    Mitoxantrone-d8 hydrochloride
    		Inhibitor
    Mitoxantrone-d8 (hydrochloride) (Mitozantrone-d8 (hydrochloride)) is deuterium labeled Mitoxantrone (dihydrochloride). Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity. Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.
    Mitoxantrone-d<sub>8</sub> hydrochloride
  • HY-13062R
    Daunorubicin hydrochloride (Standard)
    		Inhibitor
    Daunorubicin (hydrochloride) (Standard) is the analytical standard of Daunorubicin (hydrochloride). This product is intended for research and analytical applications. Daunorubicin (Daunomycin) hydrochloride is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin hydrochloride inhibits DNA and RNA synthesis. Daunorubicin hydrochloride is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin hydrochloride is also an anthracycline antibiotic. Daunorubicin hydrochloride can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
    Daunorubicin hydrochloride (Standard)
  • HY-117543
    Ethonafide
    		Inhibitor
    Ethonafide (AMP-53) is an anthracene-containing derivative of Amonafide that belongs to the Azonafide series of anticancer agents. Ethonafide (AMP-53) inhibits topoisomerase II activity by stabilizing the enzyme-DNA complex, involving both topoisomerase IIα and β.
    Ethonafide
  • HY-16742BR
    Gepotidacin mesylate hydrate (Standard)
    		Inhibitor
    Niacin (Standard) is the analytical standard of Niacin. This product is intended for research and analytical applications. Niacin (Vitamin B3) is an orally active water-soluble B3 vitamin that is an essential nutrient for humans. Niacin (Vitamin B3) plays a key role in energy metabolism, cell signaling cascades regulating gene expression and apoptosis. Niacin (Vitamin B3) is also used in the study of cardiovascular diseases.
    Gepotidacin mesylate hydrate (Standard)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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