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-132164
    Gly-7-MAD-MDCPT
    		Inhibitor
    Gly-7-MAD-MDCPT (compound 4b) is an anticancer agent. Gly-7-MAD-MDCPT is a Camptothecin (HY-16560) compound, it shows cytotoxicity to various cancer cells with IC50 values of 10-1000 nM.
    Gly-7-MAD-MDCPT
  • HY-135867D
    NHC-diphosphate
    		Inhibitor 98.80%
    NHC-diphosphate is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a diphosphate form. NHC is a pyrimidine ribonucleoside and behaves as a potent anti-virus agent. NHC effectively inhibits the replication of venezuelan equine encephalitis virus (VEEV), Chikungunya virus (CHIKV) and hepatitis C virus (HCV).
    NHC-diphosphate
  • HY-14871
    Tenifatecan
    		Inhibitor 99.78%
    Tenifatecan (SN2310) is an injectable emulsion composed of vitamin E, a succinate derivative, as well as 7-ethyl-10-hydroxycamptothecin (SN-38, the active metabolite of irinotecan). Tenifatecan (SN2310) possesses anticancer activity.
    Tenifatecan
  • HY-175741
    IID432
    		Inhibitor 98.20%
    IID432 is a Trypanosoma cruzi Topoisomerase II inhibitor with an EC50 of 8  nM for Trypanosoma cruzi. IID432, a single dose of 25 mg/kg, can achieve relapse-free parasite clearance in mouse models of chronic Chagas disease. IID432 can be used for Chagas disease research.
    IID432
  • HY-174800
    ARN21929
    		Inhibitor 99.63%
    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-B0330BR
    Levofloxacin hydrochloride (Standard)
    		Inhibitor
    Levofloxacin (hydrochloride) (Standard) is the analytical standard of Levofloxacin hydrochloride (HY-B0330B). This product is intended for research and analytical applications. Levofloxacin hydrochloride is an orally active antibiotic. Levofloxacin inhibits DNA gyrase and topoisomerase IV activity, inducing Apoptosis. Levofloxacin hydrochloride has antibacterial activity against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrochloride exhibits anticancer activity against lung cancer. Levofloxacin hydrochloride has anti-acnegenic, anxiogenic, and analgesic effects. Levofloxacin hydrochloride shortens sleep duration in mice. Levofloxacin hydrochloride can be used in the research of infectious diseases (such as tuberculosis, chronic periodontitis, bacterial infections associated with stable COPD, and BK viremia) and lung cancer.
    Levofloxacin hydrochloride (Standard)
  • HY-183912
    PY-4Car2
    		Inhibitor
    PY-4Car2 is a Camptothecin (HY-16560) derivative and a topoisomerase I inhibitor. PY-4Car2 functions as a warhead conjugated via a cleavable linker to the bispecific ADC TJ101. PY-4Car2 can be used as an ADC payload for the research of cancers.
    PY-4Car2
  • HY-B0330AR
    Levofloxacin hydrate (Standard)
    		Inhibitor
    Levofloxacin (hydrate) (Standard) is the analytical standard of Levofloxacin (hydrate). This product is intended for research and analytical applications. Levofloxacin hydrate (Levofloxacin hemihydrate) is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrate inhibits the DNA gyrase and topoisomerase IV. Levofloxacin hydrate can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin hydrate shows anti-orthopoxvirus activity.
    Levofloxacin hydrate (Standard)
  • HY-16568R
    Irinotecan hydrochloride trihydrate (Standard)
    		Inhibitor
    Irinotecan (hydrochloride trihydrate) (Standard) is the analytical standard of Irinotecan (hydrochloride trihydrate). This product is intended for research and analytical applications. Irinotecan hydrochloride trihydrate ((+)-Irinotecan hydrochloride trihydrate) is a topoisomerase I inhibitor with antitumor activity.
    Irinotecan hydrochloride trihydrate (Standard)
  • HY-177683
    N-(DBCO-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan)
    N-(DBCO-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(DBCO-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
    N-(DBCO-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan)
  • HY-177681
    N-(Mal)-N-(PEG8-Val-Cit-PAB-MMAE)-N-(PEG8-Val-Cit-PAB-Exatecan)
    N-(Mal)-N-(PEG8-Val-Cit-PAB-MMAE)-N-(PEG8-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Mal)-N-(PEG8-Val-Cit-PAB-MMAE)-N-(PEG8-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
    N-(Mal)-N-(PEG8-Val-Cit-PAB-MMAE)-N-(PEG8-Val-Cit-PAB-Exatecan)
  • HY-126142
    Top1 inhibitor 1
    		Inhibitor 99.67%
    Top1 inhibitor 1 (compound 28) is a potent human topoisomerase I (Top1) inhibitor with an IC50 value of 29 nM.
    Top1 inhibitor 1
  • HY-164836
    Deruxtecan-Eribulin
    		Inhibitor
    Deruxtecan-Eribulin is a Drug-Linker Conjugates for ADC, which is composed of a linker and a toxic molecule Exatecan (HY-13631) (DNA topoisomerase I inhibitor) and Eribulin (HY-13442) (Microtubule inhibitor). Deruxtecan-Eribulin can be used for ADC synthesis.
    Deruxtecan-Eribulin
  • HY-160806
    (5-Cl)-Exatecan
    		Inhibitor
    (5-Cl)-Exatecan is a derivative of Exatecan (HY-13631) and a DNA topoisomerase inhibitor. (5-Cl)-Exatecan serves as the cytotoxic payload component in antibody-drug conjugates (ADC) targeting ROR1-positive cancers. (5-Cl)-Exatecan is applicable for the research of ROR1-positive cancers.
    (5-Cl)-Exatecan
  • HY-153185
    Decyclohexanamine-Exatecan
    		Inhibitor 98.92%
    Decyclohexanamine-Exatecan (compound a) is a Camptothecin derivative, with a structure containing Exatecan (HY-13631), which can be used as a ADC cytotoxin.
    Decyclohexanamine-Exatecan
  • HY-120679
    XK469
    		Inhibitor 98%
    XK469 (NSC 697887) is a quinoxaline-based topoisomerase II inhibitor. XK469 exhibits antiproliferative activity against neuroblastoma cells. XK469 can be used in the research of neuroblastoma.
    XK469
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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