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-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-B0147R
    Pefloxacin (Standard)
    Pefloxacin (Standard) (Pefloxacinium (Standard)) is the analytical standard of Pefloxacin (HY-B0147). This product is intended for research and analytical applications. 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 (Standard)
  • 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-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-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-178145
    Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan
    		Inhibitor
    Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan (compound 12) is a Drug-Linker Conjugate for ADC. Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan contains the ADC linker (Mc-Lys(PEG12)-Cap-Ala-Ala-PABC) (HY-178146) and a DNA topoisomerase I inhibitor Exatecan (HY-13631). Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan can be used for the development of ADC targeting HER2-positive breast cancer.
    Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan
  • HY-13631T
    (1R,9S)-Exatecan
    (1R,9S)-Exatecan (DX8951f) is the (1R,9S) stereoisomer of Exatecan (HY-13631). Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
    (1R,9S)-Exatecan
  • 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-106122
    NK-611
    		Inhibitor
    NK-611 is an epipodophyllotoxin derivative. NK-611 induces DNA double-strand breaks by inhibiting topoisomerase II (IC50 = 56 μM). NK-611 does not inhibit microtubule polymerization, thus avoiding the side effects of the parent compound, Podofilox (HY-15552). NK-611 exhibits broad-spectrum antitumor activity and demonstrates potent efficacy in in vivo models of leukemia. NK-611 can be used in cancer research.
    NK-611
  • 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-178373
    Topoisomerase I-IN-18
    		Inhibitor
    Topoisomerase I-IN-18, a derivative of Thiosemicarbazide (HY-Y0032), is a Topoisomerase I inhibitor. Topoisomerase I-IN-18 can disrupt DNA synthesis and transcription. Topoisomerase I-IN-18 inhibits tumor cell proliferation by inducing S-phase cell cycle arrest. Topoisomerase I-IN-18 can enhance mitochondria-mediated apoptosis, suppress cell migration, and increase intracellular Reactive Oxygen Species (ROS) levels. Topoisomerase I-IN-18 can increase p53 protein expression, γH2AX phosphorylation, upregulate Bax expression, downregulate Bcl-2 expression, and activate the caspase cascade. Topoisomerase I-IN-18 can be used for the study of lung cancer.
    Topoisomerase I-IN-18
  • 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
  • HY-147801
    Topoisomerase IIα-IN-3
    		Inhibitor
    Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cell cycle at the G0/G1 phase and induces apoptosis.
    Topoisomerase IIα-IN-3
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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