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-N10495
    Seconeolitsine
    		Inhibitor 98.65%
    Seconeolitsine, an antibiotic, and is an inhibitor of targeting topoisomerase I (TopA). Seconeolitsine also is a new antimicrobial agent that can inhibit S. pneumoniae growth. Seconeolitsine can inhibit TopA relaxation activity with an IC50 value of 17 μM. Seconeolitsine can be used for the research of S. pneumoniae infections resistant to other antibiotics.
    Seconeolitsine
  • HY-N2063
    12-Ethyl-9-hydroxycamptothecin
    		99.89%
    12-Ethyl-9-hydroxycamptothecin is a derivative of Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM.
    12-Ethyl-9-hydroxycamptothecin
  • HY-153797
    Dox-btn2
    		Inhibitor
    Dox-btn2 is a biotin labeled Doxorubicin (HY-15142A), with a biotin label at the point of conjugation to doxorubicin at 3'-NH2. Dox-btn2 can be used for cell imaging. While Doxorubicin is mainly accumulated in the nucleus, while Dox-btn2 is mainly located in the cytoplasm.
    Dox-btn2
  • 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-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-B0356AS1
    Ciprofloxacin-13C3,15N monohydrochloride
    		Inhibitor 99.9%
    Ciprofloxacin-13C3,15N (Bay-09867-13C3,15N) monohydrochloride is 13C- and 15N-labeled Ciprofloxacin (monohydrochloride) (HY-B0356A).
    Ciprofloxacin-<sup>13</sup>C<sub>3</sub>,<sup>15</sup>N monohydrochloride
  • HY-45157
    Exatecan Intermediate 7
    		Inhibitor 99.24%
    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-N2306A
    Aclacinomycin A hydrochloride
    		Inhibitor
    Aclacinomycin A (Aclarubicin) hydrochloride is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A hydrochloride is an inhibitor of topoisomerase I and II. Aclacinomycin A hydrochloride inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A hydrochloride might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis.
    Aclacinomycin A hydrochloride
  • HY-147307
    MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan
    		Inhibitor 99.55%
    MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan is a agent-linker conjugate for ADC, contains the ADC linker (MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic acid) and a DNA topoisomerase I inhibitor Exatecan (HY-13631). MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan synthesized ADC can be used in study of cancer.
    MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan
  • HY-N6865
    Groenlandicine
    		Agonist 99.87%
    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-148058
    Topoisomerase I inhibitor 8
    		Inhibitor 99.87%
    Topoisomerase I inhibitor 8 is a potent topoisomerase I inhibitor. Topoisomerase I inhibitor 8 is a hexacyclic analogue of camptothecin, and displays cytotoxic effect against tumor cells.
    Topoisomerase I inhibitor 8
  • HY-132164
    Gly-7-MAD-MDCPT
    		Inhibitor
    Gly-7-MAD-MDCPT (compound 4b) is an anticancer agent. Gly-7-MAD-MDCPT is a Camptothecin (HY-16560) compound, it shows cytotoxicity to various cancer cells with IC50 values of 10-1000 nM.
    Gly-7-MAD-MDCPT
  • HY-160774
    Val-Cit-PABC-DOX
    		Inhibitor
    Val-Cit-PABC-DOX (compound 10109), an epsilon-poly-L-lysine-based drug conjugate, is an agent-linker conjugate for ADC by using a DNA topoisomerase I and topoisomerase II inhibitor, Doxorubicin (HY-15142), linked via the linker, Val-Cit-PABC.
    Val-Cit-PABC-DOX
  • 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-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-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-160649
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan
    		Inhibitor 99.72%
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan is an agent linker conjugate for ADC, with an inhibitor for Topoisomerase Exatecan (HY-13631) with IC50 of 22 μM. MC-Gly-Gly-Phe-Gly-GABA-Exatecan targets various antibodies, exhibits cytotoxic and antitumor efficacy in vitro and in vivo.
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan
  • HY-13622
    Elomotecan hydrochloride
    		Inhibitor
    Elomotecan hydrochloride (BN 80927) is a potent inhibitor of topoisomerases I and II. Elomotecan hydrochloride (BN 80927) is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan hydrochloride (BN 80927) reduces the proliferation of different tumor cells with higher potency than other anticancer agents of reference targeting topoisomerases I and II.
    Elomotecan hydrochloride
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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