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-RS14891
    Top1 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Top1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Top1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Top1 Mouse Pre-designed siRNA Set A
  • HY-146189
    Topoisomerase II inhibitor 9
    		Inhibitor
    Topoisomerase II inhibitor 9 (Compound 19b) is a Topo II inhibitor with an IC50 of 0.97 μM. Topoisomerase II inhibitor 9 is also a classical DNA-intercalator with an IC50 of 43.51 μM. Topoisomerase II inhibitor 9 arrests the cell cycle at the G2/M phase and induces apoptosis in Hep G‐2 cells.
    Topoisomerase II inhibitor 9
  • HY-156516
    10NH2-11F-Camptothecin
    		Inhibitor
    10NH2-11F-Camptothecin is a Camptothecin (HY-16560) analogue that serves as an ADC cytotoxin for the synthesis of antibody-drug conjugates (ADCs). 10NH2-11F-Camptothecin can inhibit tumor growth and is used in cancer research.
    10NH2-11F-Camptothecin
  • HY-150685
    Topo I/COX-2-IN-1
    		Inhibitor
    Topo I/COX-2-IN-1 (1H-30) is a potential Topo I/COX-2 inhibitor. Topo I/COX-2-IN-1 inhibits COX-2 and Topo I with the IC50 value of 0.24 μM and 4.42 μM, respectively. Topo I/COX-2-IN-1 can induce apoptosis and inhibit migration of cancer cells, has anti-cancer activity.
    Topo I/COX-2-IN-1
  • HY-19437
    Bimolane
    		Inhibitor
    Bimolane (AT-1727), a human topoisomerase II inhibitor, can be used as an anti-neoplastic agent and for the research of psoriasis. Bimolane shows leukemogenic activity and induces multiple types of chromosomal aberrations in human lymphocytes.
    Bimolane
  • HY-176762
    TOP3B-IN-1
    		Inhibitor
    TOP3B-IN-1 (NSC-260610) is a Topoisomerase IIIβ (TOP3B) inhibitor. TOP3B-IN-1 fails to induce the formation of TOP3B cleavage complexes (TOP3Bccs) with both DNA and RNA, and destabilizes TOP3Bccs. TOP3B-IN-1 can be used as a control compound for the development of inhibitors targeting TOP3B.
    TOP3B-IN-1
  • HY-125930A
    T-2513 hydrochloride
    		Inhibitor
    T-2513 hydrochloride is a selective topoisomerase I inhibitor. T-2513 hydrochloride binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death.
    T-2513 hydrochloride
  • HY-169299
    TOPOI/PARP-1-IN-2
    		Inhibitor
    TOPOI/PARP-1-IN-2 (compound 6c) is a dual PARP-1 and topoisomerase 1 (TOPO-1) inhibitor with IC50s of 32.2 nM and 46.2 nM, respectively. TOPOI/PARP-1-IN-2 shows a selectivity for PARP-1 over PARP-2. TOPOI/PARP-1-IN-2 disrupts the cell cycle at the S phase and induces apoptosis in NCI-60 cancer cell lines.
    TOPOI/PARP-1-IN-2
  • HY-150755
    Topo I/COX-2-IN-2
    		Inhibitor
    Topo I/COX-2-IN-2 (Compound W10) is a potent dual-target inhibitor of Topo I and COX-2 with IC50 values of 0.90 μM and 2.31 μM, respectively. Topo I/COX-2-IN-2 induces cancer cell apoptosis through the mitochondrial pathway.
    Topo I/COX-2-IN-2
  • HY-126333
    Topoisomerase II inhibitor 1
    		Inhibitor
    Topoisomerase II inhibitor 1 (compound 89) is a highly efficient and selective topoisomerase IIα inhibitor.
    Topoisomerase II inhibitor 1
  • HY-147861
    Topoisomerase II inhibitor 11
    		Inhibitor
    Topoisomerase II inhibitor 11 (compound 3d) is a potent Topoisomerase II inhibitor, with an IC50 of 2.89 μM. Topoisomerase II inhibitor 11 shows 92.46% inhibition on renal cancer cell line A498 with an IC50 of 3.5 μM. Topoisomerase II inhibitor 11 causes cell cycle arrest at the G2/M phase leading to cell proliferation inhibition and pro-apoptotic activity.
    Topoisomerase II inhibitor 11
  • HY-119827
    Moflomycin
    		Agonist
    Moflomycin (F 860191) is a compound with strong anti-leukemic activity and low mutagenicity. Moflomycin has an antiproliferative effect on the leukemic cell line HL60 in vitro (IC50=2.9 nM). Moflomycin enhances topoisomerase II-induced DNA breaks and free radical production.
    Moflomycin
  • HY-137005
    CS1
    		Inhibitor
    CS1 is a potent DNA Topo II α inhibitor. CS1 displays broad-spectrum in vitro antitumor effects, low toxicity in vivo and potential anti-multidrug resistance capabilities. CS1 leads to DNA damage, cell cycle arrest at G2/M phase and apoptosis.
    CS1
  • HY-N2331R
    Proscillaridin A (Standard)
    		Inhibitor
    Proscillaridin A (Standard) is the analytical standard of Proscillaridin A. This product is intended for research and analytical applications. Proscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively.
    Proscillaridin A (Standard)
  • HY-125930
    T-2513
    		Inhibitor
    T-2513 is a selective topoisomerase I inhibitor. T-2513 binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death.
    T-2513
  • HY-162271
    Antibacterial agent 187
    Antibacterial agent 187 (IKE7) is a derivative containing imidazole and triazolacridone structures that target yeast topoisomerase II. Antibacterial agent 187 has antifungal activity and MIC value of resistance to fluconazole (HY-B0101) is 32-64 μg/mL.
    Antibacterial agent 187
  • HY-161970
    XSJ05
    		Inhibitor
    XSJ05 is a camptothecin (CPT) derivative that can inhibit topoisomerase I (Topo I) to exert anti-cancer activity. XSJ05 can trigger DNA double-strand breaks, leading to DNA damage. XSJ05 can inhibit the growth of colorectal cancer (CRC), arrest the cell cycle in G2/M phase, and induce apoptosis.
    XSJ05
  • HY-123143
    XR11576
    		Inhibitor
    XR11576 (MLN576) is an orally active inhibitor of topoisomerase I and II. XR11576 shows cytotoxicity against human and murine tumor cell lines (IC50: 6-47 nM).
    XR11576
  • HY-159966
    Top/HDAC-IN-3
    		Inhibitor
    Top/HDAC-IN-3 (Compound 31) is an orally active dual inhibitor of Topoisomerase and HDAC. Top/HDAC-IN-3 increases reactive oxygen species (ROS) levels, leading to DNA damage, thereby inhibiting cancer cell colony formation and migration, inducing cancer cell Apoptosis, and causing cell cycle arrest. In the NSCLC model, Top/HDAC-IN-3 exhibited significant antitumor effects, with a tumor growth inhibition (TGI) of 77.5% at 100 mg/kg, surpassing the efficacy of the HDAC inhibitor SAHA (HY-10221) and the combination of SAHA (HY-10221) with the topoisomerase inhibitor Irinotecan (HY-16562).
    Top/HDAC-IN-3
  • HY-119425
    Razoxane
    		Inhibitor 99.16%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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