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-114668
    Camptothecin-20(S)-O-propionate
    		Inhibitor 99.55%
    Camptothecin-20(S)-O-propionate (CZ48), the C20-propionate ester of CPT, is a highly effective anticancer agent. Camptothecin-20(S)-O-propionate (CZ48) is a topoisomerase-Ι inhibitor.
    Camptothecin-20(S)-O-propionate
  • HY-153031A
    Val-Cit-PAB-Exatecan TFA
    		Inhibitor 99.73%
    Val-Cit-PAB-Exatecan (Val-Cit-PAB-DX8951) TFA is a agent-linker conjugate for ADC. Val-Cit-PAB-Exatecan TFA is composed of a DNA topoisomerase I DX-8951 (HY-13631) and a cathepsin cleavable ADC linker.
    Val-Cit-PAB-Exatecan TFA
  • HY-128995AS
    Glycyl-Exatecan-d5 hydrochloride
    		Inhibitor
    Glycyl-Exatecan-d5 (Glycyl-DX-8951-d5) hydrochloride is deuterium labeled Glycyl-Exatecan (HY-128995A). Glycyl-Exatecan (Glycyl-DX-8951), a derivative of Exatecan (HY-13631), is an anticancer agent. Glycyl-Exatecan has significantly antitumor activity. Glycyl-Exatecan can be used for cancers like solid tumors research.
    Glycyl-Exatecan-d<sub>5</sub> hydrochloride
  • HY-13768
    Topotecan
    		Inhibitor
    Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity.
    Topotecan
  • 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-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-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-B0147
    Pefloxacin
    		99.79%
    Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies.
    Pefloxacin
  • 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-150402
    MC-Gly-Gly-Phe-Gly-amide-cyclopropanol-amide-Exatecan
    		Inhibitor 99.16%
    MC-Gly-Gly-Phe-Gly-amide-cyclopropanol-amide-Exatecan is a pharmaceutical composition containing antibody agent conjugate (ADC). (extracted from patent WO2021190581 Example 1-8).
    MC-Gly-Gly-Phe-Gly-amide-cyclopropanol-amide-Exatecan
  • 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-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-153401
    Topoisomerase II inhibitor 13
    		Inhibitor 98.07%
    Topoisomerase II inhibitor 13 is a topoisomerase II (Topo II) inhibitor. Topoisomerase II inhibitor 13 shows antiproliferative activity against several cancer cells. Topoisomerase II inhibitor 13 induces cancer cells apoptosis.
    Topoisomerase II inhibitor 13
  • 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-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-106410A
    Zabofloxacin hydrochloride
    		Inhibitor 99.54%
    Zabofloxacin hydrochloride (DW-224a) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin hydrochloride has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia. Zabofloxacin hydrochloride is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP).
    Zabofloxacin hydrochloride
  • HY-101775A
    9-Hydroxyellipticine hydrochloride
    		Inhibitor 99.0%
    9-Hydroxyellipticine hydrochloride is a inhibitor of Topo II and RyR. 9-Hydroxyellipticine hydrochloride exhibits antitumor, antioxidant and catecholamine-releasing activities. 9-Hydroxyellipticine hydrochloride exhibits IC50 values of 1.6 μM and 1.2μM in Hela S-3 and 293T cells, respectively.
    9-Hydroxyellipticine hydrochloride
  • HY-19637
    SW044248
    		Inhibitor 99.60%
    SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.
    SW044248
  • HY-147408
    Rezetecán
    		Inhibitor 99.60%
    Rezetecán (SHR9265) is a topoisomerase I inhibitor. In addition, Rezetecán can be used to synthesize Trastuzumab rezetecan, an antineoplastic agent. Rezetecán can be used as a cytotoxic payload (ADC Cytotoxin) in antibody-drug conjugates (ADCs).
    Rezetecán
  • 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)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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