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-174800
    ARN21929
    		Inhibitor
    ARN21929 is a Topoisomerase II inhibitor with an IC50 of 4.5 μM. ARN21929 exhibits excellent kinetic and thermodynamic solubility as well as metabolic stability. However, ARN21929 shows poor antiproliferative activity against A549, DU145, MCF7, HeLa, and A375 cells. ARN21929 can be used in the study of cancer.
    ARN21929
  • HY-107096
    CH-0793076
    		Inhibitor
    CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein).
    CH-0793076
  • HY-135867
    NHC-triphosphate
    		Inhibitor 99.80%
    NHC-triphosphate is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a triphosphate form. NHC-triphosphate is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA.
    NHC-triphosphate
  • HY-121649
    AQ4
    		Inhibitor
    AQ4 is a topoisomerase II inhibitor and DNA intercalator as a chemically stable cytotoxic agent in many human tumor lines.
    AQ4
  • HY-W897655
    20-O-Acetylcamptothecin
    		Inhibitor
    20-O-Acetylcamptothecin (O-Acetylcamptothecin) is a derivative of Camptothecin (HY-16560) and an inhibitor of Topoisomerase I.
    20-O-Acetylcamptothecin
  • HY-171931A
    Aminocaproyl-Val-Cit-PABC-Exatecan TFA
    		Inhibitor 99.18%
    Aminocaproyl-Val-Cit-PABC-Exatecan TFA is a drug-linker conjugate for ADC, consiting of a cleavable linker (Aminocaproyl-Val-Cit-PABC) and Exatecan (HY-13631) (topoisomerase I inhibitor). Aminocaproyl-Val-Cit-PABC-Exatecan TFA can be used for ADC molecues synthesis.
    Aminocaproyl-Val-Cit-PABC-Exatecan TFA
  • HY-158329
    Alloc-DOX
    		Inhibitor 98.40%
    Alloc-DOX (N-Alloc doxorubicin) is a Doxorubicin (HY-15142A) prodrug. The combination of a catalyst (such as nano-palladium) and alloc-DOX leads to a decrease in cell viability and tumour growth.
    Alloc-DOX
  • HY-13618
    Edotecarin
    		Inhibitor 98.39%
    Edotecarin is a potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage, with IC50 of 50 nM.
    Edotecarin
  • HY-107096B
    CH-0793076 TFA
    		Inhibitor 98.71%
    CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein).
    CH-0793076 TFA
  • HY-106410
    Zabofloxacin
    		Inhibitor 98.02%
    Zabofloxacin (DW-224a Free base) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia. Zabofloxacin is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP).
    Zabofloxacin
  • HY-171931
    Aminocaproyl-Val-Cit-PABC-Exatecan
    		Inhibitor
    Aminocaproyl-Val-Cit-PABC-Exatecan is a drug-linker conjugate for ADC, consiting of a cleavable linker (Aminocaproyl-Val-Cit-PABC) and Exatecan (HY-13631) (topoisomerase I inhibitor). Aminocaproyl-Val-Cit-PABC-Exatecan can be used for ADC molecues synthesis.
    Aminocaproyl-Val-Cit-PABC-Exatecan
  • HY-132164B
    Gly-7-MAD-MDCPT TFA
    		Inhibitor
    Gly-7-MAD-MDCPT (Compound 4b) TFA is an anticancer agent. Gly-7-MAD-MDCPT TFA is a Camptothecin (HY-16560) compound, which shows cytotoxicity to various cancer cells with IC50 values of 10-1000 nM.
    Gly-7-MAD-MDCPT TFA
  • HY-10529R
    Betulinic acid (Standard)
    		Inhibitor
    Betulinic acid (Standard) is the analytical standard of Betulinic acid. This product is intended for research and analytical applications. Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties.
    Betulinic acid (Standard)
  • HY-43565B
    Exatecan intermediate 10
    		Inhibitor 99.92%
    Exatecan intermediate 10 is an intermediate in the synthesis of Exatecan (HY-13631).Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 of 2.2 μM (0.975 μg/mL) for use in cancer research.
    Exatecan intermediate 10
  • HY-106582
    Sobuzoxane
    		Inhibitor 98.05%
    Sobuzoxane (MST-16) is an orally active topoisomerase II inhibitor. Sobuzoxane causes irreversible inhibition of cell division. Sobuzoxane can be used in the study of non-Hodgkin's lymphoma that is resistant to conventional chemotherapy or has recurred.
    Sobuzoxane
  • HY-13620
    Elinafide
    		Inhibitor 98.59%
    Elinafide is an anticancer agent with a naphthalimide structure that targets DNA. Elinafide interferes with cell metabolism by inserting a planar ring into the DNA double helix and interacting with enzymes through its side chain.LU-79553 is a DNA-binding topoisomerase II inhibitor. The IC50 value of Elinafide for HT-29 cells is 0.014 μM.
    Elinafide
  • HY-B0067A
    Amrubicin hydrochloride
    		Inhibitor 98.78%
    Amrubicin (SM-5887) hydrochloride is a DNA topoisomerase II inhibitor, used for the research of cancer.
    Amrubicin hydrochloride
  • 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-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-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)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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