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-45157
    Exatecan Intermediate 7
    		Inhibitor
    Exatecan Intermediate 7 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 7 can be used to synthesize Antibody-Drug Conjugates (ADCs).
    Exatecan Intermediate 7
  • HY-171747
    AMT-562
    		Inhibitor
    AMT-562 is an antibody-drug conjugate (ADC) consisting of a novel anti-HER3 antibody Ab562 (HY-P991505) conjugated to the linker MC-VA-PAB and the topoisomerase I inhibitor Exatecan (HY-13631). The ADC toxic molecule and linker portion are MC-VA-PAB-Exatecan (HY-147270). AMT-562 can induce apoptosis and has antitumor activity against pancreatic, esophageal, and gastric cancers.
    AMT-562
  • HY-B0879
    Suramin
    		Inhibitor
    Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor.Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
    Suramin
  • 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-135867A
    NHC-triphosphate tetrasodium
    		Inhibitor
    NHC-triphosphate tetrasodium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a triphosphate form. NHC-triphosphate tetrasodium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA.
    NHC-triphosphate tetrasodium
  • HY-148668A
    MC-Gly-Gly-Phe-Gly-(S)-Cyclopropane-Exatecan
    		Inhibitor 98.99%
    MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan is a agent-linker conjugates for ADC, consisting Exatecan (HY-13631). Exatecan is a DNA Topoisomerase I inhibitor (IC50=2.2 μM).
    MC-Gly-Gly-Phe-Gly-(S)-Cyclopropane-Exatecan
  • HY-123393
    PNU-142586
    		Inhibitor
    PNU-142586 is the major metabolite of Linezolid (HY-10394). PNU-142586 can inhibit the activity of DNA topoisomerase 2-α (TOP2A) and DNA topoisomerase 2-β (TOP2B). PNU-142586 interferes with DNA replication and transcription by blocking the binding of DNA to TOP2 and inhibiting ATP hydrolysis, ultimately leading to antiproliferative and cytotoxic effects, including mitochondrial dysfunction. PNU-142586 can be used to study Linezolid-induced hematotoxicity and its molecular mechanism.
    PNU-142586
  • HY-119425
    Razoxane
    		Inhibitor 99.78%
    Razoxane (ICRF 159), a EDTA (HY-Y0682) derivative, is an orally active antiangiogenic topoisomerase II inhibitor. Razoxane has antineoplastic, antiangiogenic, and antimetastatic activities. Razoxanecan be used for the research of renal cell carcinoma (RCC), lung cancer and melanoma cancer.
    Razoxane
  • HY-171138
    Mal-VC-PAB-DMEA-PNU-159682
    		Inhibitor 99.36%
    Mal-VC-PAB-DMEA-PNU-159682 is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-topoisomerase II agent, PNU-159682, linked via the lysosomally cleavable dipeptide, Mc-VC-PAB. Mal-VC-PAB-DMEA-PNU-159682 can be used in the synthesis of Anti-CD22-NMS249 (HY-164761).
    Mal-VC-PAB-DMEA-PNU-159682
  • HY-145397S
    (4-NH2)-Exatecan-d5
    		Inhibitor 98.62%
    (4-NH2)-Exatecan-d5 is a deuterated labeled (4-NH2)-Exatecan. (4-NH2)-Exatecan (compound A), a topoisomerase inhibitor, is a derivative of Exatecan. (4-NH2)-Exatecan can be used in the synthesis of antibody-drug conjugates (ADCs).
    (4-NH2)-Exatecan-d<sup>5</sup>
  • HY-156849
    Exatecan-methylacetamide-OH
    		Inhibitor
    Exatecan-methylacetamide-OH (compound 6) is a Exatecan derivative with anticancer effects. Exatecan-methylacetamide-OH is an ADC cytotoxin that can be used to synthesize Antibody-Drug Conjugates (ADCs) (CN112125915A; compound 6).
    Exatecan-methylacetamide-OH
  • 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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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