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-N10367
    Corydamine
    		Inhibitor
    Corydamine, 3-arylisoquinoline alkaloid, is a potent DNA topoisomerase I/II inhibitor. Corydamine has anti-cancer activity.
    Corydamine
  • HY-143301
    Topoisomerase I inhibitor 4
    		Inhibitor
    Topoisomerase I inhibitor 4 (compound 7a) is a topoisomerase I inhibitor. Topoisomerase I inhibitor 4 inhibits HepG2, A549, MCF-7 and HeLa cancer cells proliferation with IC50s of 1.20, 2.09, 1.56 and 1.92 μM, respectively. Topoisomerase I inhibitor 4 can be used for the research of cancer.
    Topoisomerase I inhibitor 4
  • HY-150045
    TP0480066
    		Inhibitor
    TP0480066 is a selective topoisomerase II inhibitor with IC50s of 1.10 and 62.89 nM for DNA gyrase and topo IV, respectively. TP0480066 shows good activity of againsting various bacterial species including drug-resistant strains. TP0480066 also exhibits potent inhibitory activity to N. gonorrhoeae, can be used in study of gonorrhea.
    TP0480066
  • HY-N8473
    Pericosine A
    		Inhibitor
    Pericosine A ((+)-Pericosine A) is a topoisomerase II (Topoisomerase II) inhibitor that can be isolated from the Periconia byssoides strain. Pericosine A has significant antitumor activity in vitro and in vivo and can be used in cancer research. Pericosine A also inhibits the protein kinase epidermal growth factor receptor.
    Pericosine A
  • HY-182759
    MN33-47
    		Degrader
    MN33-47 is a multi-target anti-tumor compound with broad-spectrum anti-proliferative activity. MN33-47 relieves the inhibition of the mitochondrial apoptosis pathway by downregulating the anti-apoptotic protein Bcl-2, while activating caspase-3 and inhibiting Topoisomerase I activity, thereby promoting its degradation through the ubiquitin-proteasome and autophagy-lysosome pathways. MN33-47 can also induce DNA cross-linking and G2/M cell cycle arrest, inhibit cancer cell migration and activate the mitochondrial apoptosis pathway, thus exerting potent anti-tumor effects. MN33-47 can improve the water solubility of SN-38 (HY-13704), and exhibits dose-dependent tumor growth inhibition effects in CT26 tumor-bearing mouse models without obvious toxic and side effects. MN33-47 can be used in related studies on colorectal adenocarcinoma, cervical adenocarcinoma, hepatocellular carcinoma, alveolar basal epithelial adenocarcinoma, gastric cancer and colon cancer.
    MN33-47
  • HY-B0147S
    Pefloxacin-d5
    		98.33%
    Pefloxacin-d5 (Pefloxacinium-d5) is the deuterium labeled Pefloxacin (HY-B0147). Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies.
    Pefloxacin-d<sub>5</sub>
  • HY-153069A
    GGFG-PAB-Exatecan TFA
    		Inhibitor
    GGFG-PAB-Exatecan TFA consists of an ADC toxin Exatecan (HY-13631) and a linker GGFG-PAB, and can be used as a drug-linker conjugate for the synthesis of ADC molecules.
    GGFG-PAB-Exatecan TFA
  • HY-79490S
    Ac-Exatecan-d5
    		Inhibitor 99.93%
    Ac-Exatecan-d5 is the deuterium labeled Ac-Exatecan (HY-79490).
    Ac-Exatecan-d<sub>5</sub>
  • HY-175589
    XSJ81
    		Inhibitor
    XSJ81 is an orally active anti-cancer agent. XSJ81 significantly inhibits the proliferation of ampullary carcinoma (AC) DPC-X3 cells with an IC50 of 0.655 μM. XSJ81 inhibits the colony formation, arrests cell cycle at the G2/M phase and inhibits the migration in DPC-X3 cells. XSJ81 induces DNA damage and apoptosis in DPC-X3 cells. XSJ81 demonstrates significant anti-tumor efficacy in mice bearing DPC-X3 xenografts. XSJ81 can be used for the study of ampullary carcinoma.
    XSJ81
  • HY-161385
    Topoisomerase I inhibitor 16
    		Inhibitor
    Topoisomerase I inhibitor 21 (Compound 3e) is an inhibitor for Topoisomerase I through stabilization of enzyme-DNA complex. Topoisomerase I inhibitor 21 exhibits antiproliferative activity in 39 human cancer cells (JFCR39) with mean GI50 39 nM.
    Topoisomerase I inhibitor 16
  • HY-N6714R
    Alternariol (Standard)
    		Inhibitor
    Alternariol (Standard) is the analytical standard of Alternariol. This product is intended for research and analytical applications. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects.
    Alternariol (Standard)
  • HY-135845
    TP3011
    		Inhibitor
    TP3011 (CH0793011) is an active metabolite of CH-0793076 and is a potent topoisomerase I inhibitor equipotent as SN38. TP3011 is against cancer cell lines growth with IC50s at the range sub-nanomolar in vitro.
    TP3011
  • HY-149309
    Topoisomerase inhibitor 2
    		Inhibitor
    Topoisomerase inhibitor 2 (18C) is a bacterial topoisomeraseinhibitor that exhibits potent broad-spectrum activity against multidrug-resistant Gram-negative bacteria.
    Topoisomerase inhibitor 2
  • HY-143278
    FLT3-IN-13
    		Inhibitor
    FLT3-IN-13 (compound 20) is a potent and effective antileukemic topoisomerase II and FLT3 dual inhibitor with IC50 values of 2.26 μM and 2.26 μM, respectively. FLT3-IN-13 arrests cell cycle at G2/M phase and induce apoptosis. FLT3-IN-13 has anticytotoxic activity, particularly against leukemia.
    FLT3-IN-13
  • HY-159935
    Top1-IN-2
    		Inhibitor
    Top1-IN-2 (Compound 1a) is a topoisomerase 1 (Top1) inhibitor. Top1-IN-2 inhibits P-gp resistant tumor cells growth and induces cell apoptosis.
    Top1-IN-2
  • HY-146188
    Topoisomerase II inhibitor 8
    		Inhibitor
    Topoisomerase II inhibitor 8 (compound 22) is a potent topoisomerase II inhibitor, with an IC50 of 0.52 μM. Topoisomerase II inhibitor 8 exhibits good anti-proliferative activities and can arrest the cell cycle at G2/M phase.
    Topoisomerase II inhibitor 8
  • HY-W665464
    (Rac)-7-Ethyl-10-hydroxycamptothecin
    		Inhibitor
    (Rac)-7-Ethyl-10-hydroxycamptothecin is the derivative of (±)-10-Hydroxycamptothecin (HY-N0275). (±)-10-Hydroxycamptothecin is an indole alkaloid that inhibits the activity of topoisomerase I and has a broad spectrum of anticancer activity.
    (Rac)-7-Ethyl-10-hydroxycamptothecin
  • HY-W744235
    Levofloxacin-d3 sodium
    Levofloxacin-d3 sodium is the deuterium labeled Levofloxacin sodium (HY-B0330C). Levofloxacin ((-)-Ofloxacin) sodium is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin sodium inhibits the DNA gyrase and topoisomerase IV. Levofloxacin sodium can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin sodium shows anti-orthopoxvirus activity.
    Levofloxacin-d<sub>3</sub> sodium
  • HY-146504
    Topoisomerase I/II inhibitor 3
    		Inhibitor
    Topoisomerase I/II inhibitor 3 (compound 7) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis by inhibiting PI3K/Akt/mTOR signaling pathway. Topoisomerase I/II inhibitor 3 can be used for liver cancer research.
    Topoisomerase I/II inhibitor 3
  • HY-169106
    Topoisomerase inhibitor 4
    		Inhibitor
    Topoisomerase inhibitor 4 (compound 45) is a potent Topoisomerase1/2 inhibitor. Topoisomerase inhibitor 4 causes cell cycle arrest in the G2/M phase by inducing Apoptosis. Topoisomerase inhibitor 4 has antitumor activity.
    Topoisomerase inhibitor 4
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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