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-109855
    CP-67015
    		Inhibitor
    CP-67015, a quinolone antibiotic, is a potent topoisomerase II inhibitor. CP-67015 is a positive direct-acting mutagen in mammalian cells with both gene and chromosomal level effects.
    CP-67015
  • HY-156670
    Camptothecin analog-1
    Camptothecin analog-1 (Comp 166) is a camptothecin analog.
    Camptothecin analog-1
  • HY-13704S2
    SN-38-13C6
    		Inhibitor
    SN-38-13C6 (7-Ethyl-10-hydroxycamptothecin-13C6) is the 13C-labeled SN-38 (HY-13704). SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 can bind to RPL15. 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-<sup>13</sup>C<sub>6</sub>
  • HY-E70901
    Topoisomerase II α, Human
    Topoisomerase II α, Human (EC 5.99.1.3) is a nuclear enzyme that play essential roles in DNA replication, transcription, chromosome segregation, and recombination. All cells have two major forms of topoisomerases: type I, which makes single-stranded cuts in DNA, and type II enzymes, which cut and pass double-stranded DNA.
    Topoisomerase II α, Human
  • HY-105293
    NSC 727357
    		Inhibitor
    NSC 727357 is a DNA intercalator and topoisomerase inhibitor with antitumor activity. NSC 727357 can inhibit cells proliferation and induce G1 phase arrest. NSC 727357 can be used for the research of cancer, such as melanoma.
    NSC 727357
  • HY-161628
    Tapcin
    		Inhibitor
    Tapcin is a dual inhibitor for topoisomerase I and topoisomerase II, with IC50 of 203 and 71 nM. Tapcin inhibits proliferations of cancer cells A-375, HeLa, Huh7.5, U2-OS, A549, Caco-2 and HT29, with IC50s of 441, 1.04, 40.5, 0.002, 0.006, 0.287 and 0.842 nM, respectively. Tapcin exhibits antitumor activity in HT29 xenograft model.
    Tapcin
  • HY-16562AR
    Irinotecan hydrochloride (Standard)
    		Inhibitor
    Irinotecan (hydrochloride) (Standard) is the analytical standard of Irinotecan (hydrochloride). This product is intended for research and analytical applications. Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer.
    Irinotecan hydrochloride (Standard)
  • HY-145291
    CPT-Se4
    		Inhibitor
    CPT-Se4, a selenoproagent of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT-Se4 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se4 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC50= 2.54-6.4 μM).
    CPT-Se4
  • HY-101959
    Tyrphostin AG213
    		Inhibitor
    Tyrphostin AG213 (AG213) is an inhibitor of epidermal growth factor receptor (EGFR) protein tyrosine kinase (IC50=0.85 μM). Tyrphostin AG213 inhibits tyrosine kinase activity IC50=2.4 μM) and topoisomerase II (IC100=50 μM). Tyrphostin AG213 can induce nonapoptotic cell programmed death in tumor cells.
    Tyrphostin AG213
  • HY-118036
    ACT-387042
    		Inhibitor
    ACT-387042 is a bacterial topoisomerase inhibitor with broad-spectrum activity against Gram-positive and Gram-negative bacteria, including methicillin-resistant Staphylococcus aureus and penicillin- and fluoroquinolone-resistant Streptococcus pneumoniae .
    ACT-387042
  • HY-183090
    EGFR/VEGFR2-IN-13
    		Inducer
    EGFR/VEGFR2-IN-13 is a multi-target inhibitor, with an IC50 of 0.98 µM against VEGFR-2, 1.01 µM against EGFR, and 1.94 µM against topoisomerase II. EGFR/VEGFR2-IN-13 induces cell cycle arrest and apoptosis in tumor cells. As an anticancer agent, EGFR/VEGFR2-IN-13 exhibits cytotoxicity against cancer cells. EGFR/VEGFR2-IN-13 can be used in research related to breast cancer, colon cancer, and liver cancer.
    EGFR/VEGFR2-IN-13
  • HY-177687
    N-(Mal-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan)
    N-(Mal-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Mal-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
    N-(Mal-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan)
  • HY-17577R
    Berberine chloride hydrate (Standard)
    		Inhibitor
    Berberine (chloride hydrate) (Standard) is the analytical standard of Berberine (chloride hydrate). This product is intended for research and analytical applications. Berberine chloride hydrate (Natural Yellow 18 chloride hydrate) is an alkaloid that acts as an antibiotic. Berberine chloride hydrate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties[1].
    Berberine chloride hydrate (Standard)
  • HY-13768S2
    Topotecan-d6 dihydrochloride
    		Inhibitor
    Topotecan-d6 dihydrochloride (SKF 104864A-d6 dihydrochloride) is the deuterium labeled Topotecan dihydrochloride. Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity.
    Topotecan-d<sub>6</sub> dihydrochloride
  • HY-161082
    Topoisomerase I inhibitor 12
    		Inhibitor
    Topoisomerase I inhibitor 12 (compound 12), a Camptothecin (HY-16560)-based derivative, is a potent Topoisomerase I inhibitor. Topoisomerase I inhibitor 12 shows anticancer activity.
    Topoisomerase I inhibitor 12
  • HY-173001
    AuL1
    		Inhibitor
    AuL1 is an inhibitor of topoisomerase IIα (Top II) with DNA-intercalating properties. AuL1 is cytotoxic to tumor cells and can be used in the research of anticancer agents.
    AuL1
  • HY-168849
    Topoisomerase inhibitor 5
    		Inhibitor
    Topoisomerase inhibitor 5 (compound 158) is a Bacterial Topoisomerase Inhibitor inhibitor with the lowest inhibitory concentration of 0.125 μg/mL. Topoisomerase inhibitor has antituberculous activity.
    Topoisomerase inhibitor 5
  • HY-18350A
    Indimitecan hydrochloride
    		Inhibitor
    Indimitecan hydrochloride is a topoisomerase I (Top1) inhibitor with anticancer activities.
    Indimitecan hydrochloride
  • HY-158387
    Anticancer agent 214
    		Inhibitor
    Anticancer agent 214 (2) is a Camptothecin compound, with IC50 values of 2.6 nM and 15.7 nM in MCF-7 cells and MDA-MB-231 cells, respectively.
    Anticancer agent 214
  • HY-W744243
    Etoposide-d4
    Etoposide-d4 (VP-16-d4; VP-16-213-d4) is the deuterium labeled Etoposide (HY-13629). 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-d<sub>4</sub>
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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