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. 상품명 효과 Purity Chemical Structure
  • HY-43565B
    Exatecan intermediate 10
    		Inhibitor 99.91%
    Exatecan intermediate 10 is an intermediate in the synthesis of Exatecan (HY-13631).Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 of 2.2 μM (0.975 μg/mL) for use in cancer research.
    Exatecan intermediate 10
  • HY-46081
    Exatecan Intermediate 3
    		Inhibitor 99.83%
    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-W010800R
    Cholesteryl hemisuccinate (Standard)
    		Inhibitor
    Cholesteryl hemisuccinate (Standard) is the analytical standard of Cholesteryl hemisuccinate. This product is intended for research and analytical applications. Cholesteryl hemisuccinate is a with hepatoprotective an anticancer activity. Cholesteryl hemisuccinate inhibits Acetaminophen (AAP, HY-66005) hepatotoxicity, and prevents AAP-induced hepatic apoptosis and necrosis. Cholesteryl hemisuccinate inhibits DNA polymerase and DNA topoisomerase to inhibit DNA replication and repair and cell division. Thus, Cholesteryl hemisuccinate inhibits tumor growth[1][2].
    Cholesteryl hemisuccinate (Standard)
  • HY-16742B
    Gepotidacin mesylate hydrate
    		Inhibitor 99.62%
    Gepotidacin mesylate hydrate is an orally active triazaacenaphthylene antibiotic and bacterial type II topoisomerase inhibitor. Gepotidacin mesylate hydrate inhibits bacterial DNA replication by blocking topoisomerase enzymes. Gepotidacin mesylate hydrate selectively inhibits topoisomerase IV and the B subunit of DNA gyrase.
    Gepotidacin mesylate hydrate
  • HY-B0455A
    Lomefloxacin
    		Inhibitor 99.99%
    Lomefloxacin (SC47111A) is an orally active difluoroquinolone antibiotic. Lomefloxacin prevents DNA supercoiling and replication by inhibiting bacterial topoisomerase II. Lomefloxacin induces ROS production and Apoptosis. Lomefloxacin has broad-spectrum bactericidal activity against Gram-positive and Gram-negative bacteria. Lomefloxacin has anticancer effects against melanoma. Lomefloxacin can be used in the study of systemic bacterial infections (such as Salmonella typhimurium infections), skin and melanoma .
    Lomefloxacin
  • 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-176772
    QHL-1618
    QHL-1618 is a tumor microenvironment-activated drug conjugate. QHL-1618 inhibits the tumor growth in various tumor models, such as HT-1080 xenograft, CT-26 xenograft.
    QHL-1618
  • 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-N6865
    Groenlandicine
    		Agonist 99.72%
    Groenlandicine, a protoberberine alkaloid, is a cholinesterase inhibitor (AChE (IC50 = 0.54 μM), BChE (IC50 = 3.32 μM)). Groenlandicine non-competitively inhibits BACE1 (IC50 = 19.68 μM, Ki = 21.2) and inhibits RLAR (IC50 = 140.1 μM), HRAR (IC50 = 154.2 μM), and total ROS generation (IC50 = 51.78 μM) in vitro. Groenlandicine suppresses osteosarcoma cell proliferation while promoting apoptosis. Groenlandicine inhibits the tumor growth when combined with Cisplatin (HY-17394). Groenlandicine can be used for the study on osteosarcoma, Alzheimer's disease and diabetes mellitus .
    Groenlandicine
  • HY-B0147A
    Pefloxacin mesylate
    		99.73%
    Pefloxacin (Pefloxacinium) mesylate is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin mesylate inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin mesylate exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin mesylate has anti-Plasmodium yoelii infection activity. Pefloxacin mesylate increase UVA-induced edema and immunesuppression. Pefloxacin mesylate can be used for infection studies.
    Pefloxacin mesylate
  • 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
Cat. No. 상품명 / Synonyms Species Source
Cat. No. 상품명 / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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