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-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-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-153185
    Decyclohexanamine-Exatecan
    		Inhibitor 98.38%
    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-10534
    Voreloxin
    		Inhibitor 99.26%
    Voreloxin (SNS-595; Vosaroxin; AG 7352) is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.
    Voreloxin
  • 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-46081
    Exatecan Intermediate 3
    		Inhibitor
    Exatecan Intermediate 3 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 3 can be used to synthesize Antibody-Drug Conjugates (ADCs).
    Exatecan Intermediate 3
  • HY-43565
    Exatecan intermediate 9
    		Inhibitor 99.80%
    Exatecan intermediate 9 is an intermediate for the synthesis 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 intermediate 9
  • 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-128995AS
    Glycyl-Exatecan-d5 hydrochloride
    		Inhibitor
    Glycyl-Exatecan-d5 (hydrochloride) is deuterium labeled Glycyl-Exatecan.
    Glycyl-Exatecan-d<sub>5</sub> hydrochloride
  • HY-15142A
    Doxorubicin
    		Inhibitor
    Doxorubicin (Hydroxydaunorubicin), a broad-spectrum anthracycline antibiotic with cytotoxic properties, is an anti-cancer chemotherapy agent. Doxorubicin has fluorescence properties. Doxorubicin inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy. Doxorubicin inhibits human DNA topoisomerase I with an IC50 of 0.8 μM.
    Doxorubicin
  • HY-13062A
    Daunorubicin
    		Inhibitor
    Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
    Daunorubicin
  • 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-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-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-B0147
    Pefloxacin
    		99.79%
    Pefloxacin 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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