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-13727
    Pixantrone free base
    		Inhibitor
    Pixantrone (BBR 2778 (free base)), a mitoxantrone analog, is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
    Pixantrone free base
  • 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-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-106702A
    Fostriecin
    		Inhibitor
    Fostriecin is a triene antibiotic. Fostriecin is a topoisomerase II and protein phosphatase PP2A inhibitor.
    Fostriecin
  • HY-17460
    Garenoxacin
    		Inhibitor 98.62%
    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-B0398R
    Nalidixic acid (Standard)
    		Inhibitor
    Nalidixic acid (Standard) is the analytical standard of Nalidixic acid. This product is intended for research and analytical applications. 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 (Standard)
  • HY-16261A
    MC-DOXHZN
    		Inhibitor
    MC-DOXHZN ((E/Z)-Aldoxorubicin; Doxorubicin(6-maleimidocaproyl)hydrazone) is an albumin-binding proagent of Doxorubicin (HY-15142A) (DNA topoisomerase II inhibitor), with acid-sensitive properties. MC-DOXHZN can be used to synthesize ADC.
    MC-DOXHZN
  • HY-118942
    Topovale
    		Inhibitor 99.94%
    Topovale (ARC 111) is a topoisomerase I inhbitor. Topovale is an antitumor agent, and shows low nM cytotoxicity against a panel of cancer cells. Topovale induces reversible topoisomerase I (TOP1) cleavage complexes in tumor cells.
    Topovale
  • HY-18258R
    Berberine chloride (Standard)
    		Inhibitor
    Berberine (chloride) (Standard) is the analytical standard of Berberine (chloride). This product is intended for research and analytical applications. Berberine chloride is an alkaloid that acts as an antibiotic. Berberine chloride induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties.
    Berberine chloride (Standard)
  • HY-13631P
    Exatecan mesylate dihydrate
    		Inhibitor
    Exatecan (DX-8951) mesylate dihydrate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
    Exatecan mesylate dihydrate
  • HY-185372
    Mitoxantrone hydrochloride liposome
    		Inhibitor
    Mitoxantrone hydrochloride liposome is a liposome-encapsulated Mitoxantrone hydrochloride (HY-13502A) (a topoisomerase II inhibitor). Compared to regular Mitoxantrone hydrochloride, Mitoxantrone hydrochloride liposome enhances antitumor activity and prolongs drug circulation time in the body.
    Mitoxantrone hydrochloride liposome
  • HY-16261C
    Aldoxorubicin hydrochloride
    		Inhibitor
    Aldoxorubicin (INNO-206) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin hydrochloride (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
    Aldoxorubicin hydrochloride
  • HY-13768C
    Topotecan hydrochloride hydrate
    		Inhibitor
    Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity.
    Topotecan hydrochloride hydrate
  • HY-185371
    Irinotecan liposome
    		Inhibitor
    Irinotecan liposome is a liposome-encapsulated form of Irinotecan hydrochlorid (HY-16562A) (a topoisomerase I inhibitor). Compared with Irinotecan, Irinotecan liposome enhances antitumor activity, reduces drug release rate, and avoids neutropenia.
    Irinotecan liposome
  • HY-16055
    Silatecan
    		Inhibitor
    Silatecan (AR-67) is a blood-brain barrier-permeable derivative of Camptothecin (HY-16560), DNA topoisomerase I inhibitor, an anticancer agent, and a radiosensitizer. Silatecan potently radiosensitizes wild-type p53 gliomas. Silatecan can be used in research related to glioma, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer, breast cancer, cervical cancer, gastric cancer, nasopharyngeal cancer, and uterine cancer.
    Silatecan
  • HY-119892
    Batracylin
    		Inhibitor
    Batracylin (NSC320846) is a potent DNA Topoisomerases I and DNA Topoisomerases II inhibitor. Batracylin shows cytotoxicity and antiproliferative activity. Batracylin induces DNA breaks.
    Batracylin
  • HY-13745
    Sabarubicin
    		Inhibitor
    Sabarubicin is a doxorubicin disaccharide analogue with striking antitumor activity. Sabarubicin is more effective than doxorubicin as a topoisomerase II poison and stimulated DNA fragmentation at lower intracellular concentrations.
    Sabarubicin
  • HY-152965
    Biotin-doxorubicin
    		Inhibitor
    Biotin-doxorubicin is a Biotin-labeled Doxorubicin. Doxorubicin, a broad-spectrum anthracycline antibiotic, is a topoisomerase II inhibitor.
    Biotin-doxorubicin
  • HY-13630A
    Etoposide phosphate disodium
    		Inhibitor
    Etoposide phosphate disodium (BMY-40481 disodium) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate disodium is the phosphate ester proagent of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate disodium induces cell cycle arrest, apoptosis, and autophagy.
    Etoposide phosphate disodium
  • HY-13631AS1
    Exatecan-d3 mesylate
    		Inhibitor
    Exatecan-d3 (DX8951f-d3) mesylate is deuterium-labeled Exatecan mesylate (HY-13631A). Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL.
    Exatecan-d<sub>3</sub> mesylate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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