1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. Topoisomerase

Topoisomerase

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-157407
    Cyclooctyne-O-amido-PEG4-VC-PAB-Gly-Gly-NH-O-CO-Exatecan
    Inhibitor
    Cyclooctyne-O-amido-PEG4-VC-PAB-Gly-Gly-NH-O-CO-Exatecan is a drug-linker conjugate for ADC (ADC Cytotoxin: Exatecan).
    Cyclooctyne-O-amido-PEG4-VC-PAB-Gly-Gly-NH-O-CO-Exatecan
  • HY-W897655
    20-O-Acetylcamptothecin
    Inhibitor 98.0%
    20-O-Acetylcamptothecin (O-Acetylcamptothecin) is a derivative of Camptothecin (HY-16560) and an inhibitor of Topoisomerase I.
    20-O-Acetylcamptothecin
  • HY-150401
    Exatecan-amide-cyclopropanol
    Inhibitor 98.57%
    Exatecan-amide-cyclopropanol (compound 1) is a anticancer agent. Exatecan-amide-cyclopropanol shows anti-proliferation activity against SK-BR-3 and U87 cells, with IC50 values of 0.12 and 0.23 nM, respectively.
    Exatecan-amide-cyclopropanol
  • HY-158061A
    Topoisomerase II inhibitor 20 TFA
    Inhibitor
    Topoisomerase II inhibitor 20 TFA is a potent topoisomerase II inhibitor with IC50 of 0.98 µM. Topoisomerase II inhibitor 20 TFA can induce apoptosis and has broad-spectrum anticancer activity.
    Topoisomerase II inhibitor 20 TFA
  • HY-108969
    Pyrazoloacridine
    Inhibitor 98.05%
    Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment.
    Pyrazoloacridine
  • HY-120574
    TH1338
    Inhibitor 98.77%
    TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile.
    TH1338
  • HY-13620
    Elinafide
    Inhibitor 98.02%
    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-48878
    Exatecan analog 36
    Inhibitor 98.71%
    Exatecan analog 36 is a analog of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM).
    Exatecan analog 36
  • HY-13624AR
    Epirubicin hydrochloride (Standard)
    Inhibitor
    Epirubicin (hydrochloride) (Standard) is the analytical standard of Epirubicin (hydrochloride). This product is intended for research and analytical applications. Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
    Epirubicin hydrochloride (Standard)
  • HY-13758
    TAS-103
    Inhibitor 99.69%
    TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
    TAS-103
  • HY-B0356BR
    Ciprofloxacin hydrochloride monohydrate (Standard)
    Inhibitor
    Ciprofloxacin (hydrochloride monohydrate) (Standard) is the analytical standard of Ciprofloxacin (hydrochloride monohydrate). This product is intended for research and analytical applications. Ciprofloxacin (Bay-09867) hydrochloride monohydrate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin hydrochloride monohydrate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin hydrochloride monohydrate has anti-proliferative activity and induces apoptosis. Ciprofloxacin hydrochloride monohydrate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
    Ciprofloxacin hydrochloride monohydrate (Standard)
  • HY-16562S
    Irinotecan-d10
    Inhibitor 98.02%
    Irinotecan-d10 is a deuterium labeled Irinotecan ((+)-Irinotecan). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
    Irinotecan-d<sub>10</sub>
  • HY-15142A
    Doxorubicin
    Inhibitor
    Doxorubicin (Hydroxydaunorubicin), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy.
    Doxorubicin
  • HY-18258S
    Berberine-d6 chloride
    Inhibitor
    Berberine-d6 (chloride) is the deuterium labeled Berberine chloride. 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-d<sub>6</sub> chloride
  • HY-147095A
    Val-Ala-PABC-Exatecan trifluoroacetate
    Inhibitor 98.39%
    Val-Ala-PABC-Exatecan trifluoroacetate is a Drug-Linker Conjugates for ADC, consiting of a cleavable Tesirine linker (Val-Ala-PABC) and Exatecan (topoisomerase I inhibitor, HY-13631). Val-Ala-PABC-Exatecan trifluoroacetate can be used for ADC molecues synthesis, such as Mal-PEGn-amide-va-Exatecan.
    Val-Ala-PABC-Exatecan trifluoroacetate
  • HY-16560S
    Camptothecin-d5
    Inhibitor 99.61%
    Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.
    Camptothecin-d<sub>5</sub>
  • HY-13768S1
    Topotecan-d6
    Inhibitor
    Topotecan-d6 is the deuterium labeled Topotecan. Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95 μM of GSCs-U87.
    Topotecan-d<sub>6</sub>
  • HY-177879
    2-MSP-5-HA-VA-PAB-Exatecan
    Inhibitor
    2-MSP-5-HA-Val-Cit-PAB-Exatecan (A-24) is a drug-linker conjugate for ADC. 2-MSP-5-HA-Val-Cit-PAB-Exatecan consists of Exatecan (HY-13631) and a linker. 2-MSP-5-HA-Val-Cit-PAB-Exatecan can be used for synthesis of ADCs.
    2-MSP-5-HA-VA-PAB-Exatecan
  • HY-158061
    Topoisomerase II inhibitor 20
    Inhibitor 98.44%
    Topoisomerase II inhibitor 20 (Compound 3e) is a potent topoisomerase II (Topoisomerase II) inhibitor with an IC50 of 0.98 µM. Topoisomerase II inhibitor 20 induces apoptosis and has broad-spectrum anticancer activity.
    Topoisomerase II inhibitor 20
  • HY-135867F
    NHC-diphosphate triammonium
    Inhibitor 98.80%
    NHC-diphosphate triammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a diphosphate form. NHC-diphosphate triammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA.
    NHC-diphosphate triammonium
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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