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-147095
    Val-Ala-PABC-Exatecan
    		Inhibitor 99.90%
    Val-Ala-PABC-Exatecan is a Drug-Linker Conjugates for ADC, consiting of a cleavable Tesirine linker (Val-Ala-PABC) and Exatecan (HY-13631) (topoisomerase I inhibitor). Val-Ala-PABC-Exatecan can be used for ADC molecues synthesis, such as Mal-PEGn-amide-va-Exatecan.
    Val-Ala-PABC-Exatecan
  • HY-111630
    PluriSIn #2
    		Inhibitor 98.0%
    PluriSIn #2 is a selective transcriptional inhibitor of topoisomerase II α (TOP2A). PluriSIn #2 is a compound that selectively eliminates undifferentiated human pluripotent stem cells (hPSCs).
    PluriSIn #2
  • HY-B0455
    Lomefloxacin hydrochloride
    		Inhibitor 99.97%
    Lomefloxacin hydrochloride (NY-198 hydrochloride) is an orally active difluoroquinolone antibiotic. Lomefloxacin hydrochloride prevents DNA supercoiling and replication by inhibiting bacterial topoisomerase II. Lomefloxacin hydrochloride induces ROS production and Apoptosis. Lomefloxacin hydrochloride has broad-spectrum bactericidal activity against Gram-positive and Gram-negative bacteria. Lomefloxacin hydrochloride has anticancer effects against melanoma. Lomefloxacin hydrochloride can be used in the study of systemic bacterial infections (such as Salmonella typhimurium infections), skin and melanoma .
    Lomefloxacin hydrochloride
  • HY-10982
    Amonafide
    		Inhibitor 99.92%
    Amonafide is a topoisomerase II inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA.
    Amonafide
  • HY-171689
    Puxitatug samrotecan
    		Inhibitor 98.51%
    Puxitatug samrotecan (AZD 8205) is a B7-H4-directed antibody-drug conjugate (ADC) bearing a Topoisomerase I inhibitor (TOP1i) payload. Puxitatug samrotecan improves HR+/HER2- breast cancer.
    Puxitatug samrotecan
  • HY-13631F
    Gly-Gly-Phe-Gly-NH-O-CO-Exatecan hydrochloride
    		Inhibitor 99.52%
    Gly-Gly-Phe-Gly-NH-O-CO-Exatecan, as a drug-linker conjugate composed of linker Gly-Gly-Phe-Gly-NH-O-CO and Exatecan, can be used to prepare antibody conjugate drugs. Exatecan is a DNA topoisomerase I inhibitor that can be used in cancer research.
    Gly-Gly-Phe-Gly-NH-O-CO-Exatecan hydrochloride
  • HY-156617A
    (αR)-Cyclopropaneacetamide-Exatecan
    		Inhibitor 99.93%
    (αR)-Cyclopropaneacetamide-Exatecan (SHR169265) is a DNA Topoisomerase I inhibitor with enhanced membrane permeability (with an IC50 of 1.34 μM against the human DNA Topoisomerase I). (αR)-Cyclopropaneacetamide-Exatecan exerts cytotoxic effects by inhibiting the enzymatic activity of Topoisomerase I, and this anticancer effect is independent of the expression level of HER2. (αR)-Cyclopropaneacetamide-Exatecan is an ADC Cytotoxin derived from Exatecan (HY-13631), which can be used in research related to advanced cancers such as breast cancer, gastric cancer, colorectal cancer and non-small cell lung cancer.
    (αR)-Cyclopropaneacetamide-Exatecan
  • HY-B0330R
    Levofloxacin (Standard)
    		Inhibitor
    Levofloxacin (Standard) is the analytical standard of Levofloxacin. This product is intended for research and analytical applications. Levofloxacin ((-)-Ofloxacin) is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin inhibits the DNA gyrase and topoisomerase IV. Levofloxacin can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin shows anti-orthopoxvirus activity.
    Levofloxacin (Standard)
  • HY-13704R
    SN-38 (Standard)
    		Inhibitor
    SN-38 (Standard) is the analytical standard of SN-38. This product is intended for research and analytical applications. SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254).
    SN-38 (Standard)
  • HY-171124
    Tilatamig samrotecan
    		Inhibitor
    Tilatamig samrotecan (AZD9592) is an anti-EGFR/c-MET antibody-drug conjugate (ADC). Tilatamig samrotecan consists of an anti-EGFR/c-MET antibody with the drug-linker conjugate being AZ14170133 (HY-145399) (a topoisomerase I (TOP1i) inhibitor payload). Tilatamig samrotecan induces multiple DNA damage response pathway markers (like ATM, ATR, γH2AX). Tilatamig samrotecan selectively binds to EGFR and c-MET, delivering the cytotoxic payload. Tilatamig samrotecan exerts anti-tumor activity in vivo. Tilatamig samrotecan can be used for non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) research.
    Tilatamig samrotecan
  • HY-B0330B
    Levofloxacin hydrochloride
    		Inhibitor 99.99%
    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
  • HY-79490
    Ac-Exatecan
    		Inhibitor 99.02%
    Ac-Exatecan is acetylation-modified Exatecan (HY-13631). Exatecan is a common toxin component in ADC preparation (ADC cytotoxin) and an inhibitor of DNA topoisomerase I (IC50 = 2.2 μM). Exatecan has antitumor activity. Exatecan can be used as a payload for ADC. Exatecan is effective against P-glycoprotein mediated multi-drug resistant cells.
    Ac-Exatecan
  • HY-16228
    Genz-644282
    		Inhibitor 99.13%
    Genz-644282 is a non-camptothecin topoisomerase I inhibitor, used for cancer research.
    Genz-644282
  • HY-171580
    Mc-PEG4-Val-Ala-PAB-Exatecan
    		Inhibitor 99.65%
    Mc-PEG4-Val-Ala-PAB-Exatecan is a Drug-linker conjugate for ADC. Mc-PEG4-Val-Ala-PAB-Exatecan contains the ADC linker (Mc-PEG4-Val-Ala-PAB) and a DNA topoisomerase I inhibitor Exatecan (HY-13631).
    Mc-PEG4-Val-Ala-PAB-Exatecan
  • HY-B1099
    Hycanthone
    		Inhibitor 99.81%
    Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent.
    Hycanthone
  • HY-15753A
    Ellipticine hydrochloride
    		Inhibitor 99.01%
    Ellipticine (NSC 71795) hydrochloride is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.
    Ellipticine hydrochloride
  • HY-164729
    FZ-AD005
    		Inhibitor
    FZ-AD005 is a DLL3-targeting antibody-drug conjugate (ADC) with high selectivity, composed of the anti-DLL3 antibody FZ-A038 (HY-P990896), a dipeptide linker (Val-Ala), and DXd (HY-13631D). The Kd value of FZ-AD005 for human DLL3 ranges from 13.29 to 58.3 pmol/L. After binding to DLL3 on the cell surface, FZ-AD005 mediates endocytosis, and the payload DXd is released via cleavage by lysosomal cathepsins. DXd inhibits topoisomerase TopI to induce double-strand DNA breaks, cell cycle arrest and apoptosis, and FZ-AD005 exhibits bystander killing activity against adjacent DLL3-negative cells. FZ-AD005 shows stable circulation in vivo, has good tolerance and acceptable pharmacokinetic profiles in rats and cynomolgus monkeys, and effectively inhibits the growth of DLL3-expressing tumor cells. FZ-AD005 serves as a promising candidate molecule for research on small cell lung cancer and human neuroendocrine prostate cancer.
    FZ-AD005
  • HY-13629R
    Etoposide (Standard)
    		Inhibitor
    Etoposide (Standard) is the analytical standard of Etoposide. This product is intended for research and analytical applications. Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy.
    Etoposide (Standard)
  • HY-42487B
    (R)-Exatecan Intermediate 1
    		Inhibitor 99.95%
    (R)-Exatecan Intermediate 1 is a key intermediate in the synthesis of Camptothecin (HY-16560) derivatives, and can be used to prepare Exatecan mesylate (DX8951f) (HY-13631A). (R)-Exatecan Intermediate 1 enables the synthesis of Exatecan, which exhibits low sensitivity to multidrug resistance and has great value in anti-tumor research.
    (R)-Exatecan Intermediate 1
  • HY-158109
    M3554
    		Inhibitor 98.74%
    M3554 is an anti-GD2 antibody-drug conjugate (ADC) based on the humanized anti-GD2 antibody. M3554 consists of the humanized monoclonal antibody hu14.18 (K322A) (HY-P991040) linked to a topoisomerase 1 inhibitor Exatecan (HY-13631) via a cleavable β-glucuronide linker. M3554 can be used for the study of neuroblastoma, osteosarcoma or glioma.
    M3554
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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