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-153797
    Dox-btn2
    		Inhibitor 98.80%
    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-W008874
    meso-Tetra(4-pyridyl)porphine
    		Inhibitor
    meso-Tetra(4-pyridyl)porphine (Compound 10) is a porphyrin derivative. meso-Tetra(4-pyridyl)porphine is a weak inhibitor of human topoisomerase I (Top1) with an EC50 value greater than 50 µM. meso-Tetra(4-pyridyl)porphine can be used in tumor research.
    meso-Tetra(4-pyridyl)porphine
  • 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-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-178226
    PBX-7016
    		Inhibitor
    PBX-7016 is a Camptothecin (HY-16560) derivative. PBX-7016 can selectively inhibit Topoisomerase 1. PBX-7016 can specifically bind and degrade the cancer protein DDX5, thereby down-regulating the expression of anti-apoptotic proteins such as Survivin, Mcl-1, and XIAP, and promoting the apoptosis of cancer cells. PBX-7016 can be used to synthesis of ADCs.
    PBX-7016
  • 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-125331
    DRF-1042
    		Inhibitor 98.33%
    DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-agent resistance (MDR) phenotype.
    DRF-1042
  • 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-13670
    Lurtotecan
    		Inhibitor
    Lurtotecan (GI147211; OSI-211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan has anticancer effects.
    Lurtotecan
  • 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-114668
    Camptothecin-20(S)-O-propionate
    		Inhibitor 99.60%
    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-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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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