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-178036
    ZM484
    		Inhibitor
    ZM484 is a potent dual p53-MDM2/TOP1 inhibitor that exhibits antiproliferative and antitumor activity both in vitro and in vivo. ZM484 effectively upregulates p53 and MDM2 proteins and maintains TOP1 inhibitory activity by the release of camptothecin (CPT) and a potent p53-MDM2 inhibitor. ZM484 induces cell cycle arrest and apoptosis by regulating the expression of key apoptosis- and cycle-related proteins, including caspase-3, Bcl-2, and Cyclin B1. ZM484 can be used for colorectal cancer research.
    ZM484
  • HY-170912
    Topo I/II-IN-2
    		Inhibitor
    Topo I/II-IN-2 (Compound 3g) is an inhibitor of Topo I and Topo II. Topo I/II-IN-2 inhibits NCI-H446 cells and NCI-H1048 cells with IC50s of 1.30 μM and 1.42 μM, respectively. Topo I/II-IN-2 induces mitochondrial Apoptosis, mitochondrial dysfunction and activity generation. Topo I/II-IN-2 inhibits the PI3K/Akt/mTOR pathway. Topo I/II-IN-2 prevents SCLC (small cell lung cancer) cell proliferation, invasion, and migration in vitro. .
    Topo I/II-IN-2
  • HY-145867
    EGFR-IN-45
    		Inhibitor
    EGFR-IN-45 is a potent epidermal growth factor receptor (EGFR) pan inhibitor, with IC50s of 0.4 µM and 1.6 µM for EGFR and CDK2, respectively. EGFR-IN-45 also inhibit Topo I and Topo II. EGFR-IN-45 arrests cancer cells in the pre-G1 phase and induces apoptosis.
    EGFR-IN-45
  • HY-RS14892
    Top1 Rat Pre-designed siRNA Set A
    		Inhibitor

    Top1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Top1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Top1 Rat Pre-designed siRNA Set A
  • HY-N19312
    Diospyrin
    		Inhibitor
    Diospyrin is a dinaphthoquinone anticancer agent with pro-apoptotic (apoptosis) activity, glutathione S-transferase (Glutathione S-transferase) inhibitory activity, and topoisomerase (Topoisomerase) I inhibitory activity. Diospyrin is present in the heartwood of various Diospyros plants and can be used for research on Ehrlich ascites carcinoma, acute myeloid leukemia, chronic myeloid leukemia, mammary adenocarcinoma, cervical epithelial carcinoma, malignant cutaneous melanoma, laryngeal epidermoid carcinoma, human osteosarcoma, and human lymphoblastic carcinoma.
    Diospyrin
  • HY-149925
    DNA Gyrase-IN-6
    		Inhibitor
    Antibacterial agent 138 is a benzothiazole inhibitor of bacterial DNA gyrase and topoisomerase IV. Antibacterial agent 138 exhibits favorable solubility and plasma protein binding. Antibacterial agent 138 has antibacterial activity against Gram-positive and Gram-negative strains. Antibacterial agent 138 is a dual GyrB and ParE inhibitor.
    DNA Gyrase-IN-6
  • HY-16562AS
    Irinotecan-d5 hydrochloride
    		Inhibitor
    Irinotecan-d5 hydrochloride is deuterated labeled Irinotecan hydrochloride (HY-16562A). Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer.
    Irinotecan-d<sub>5</sub> hydrochloride
  • HY-156517
    7Ethanol-10NH2-11F-Camptothecin
    		Inhibitor
    7Ethanol-10NH2-11F-Camptothecin is a Camptothecin (HY-16560) analogue that serves as an ADC cytotoxin for the synthesis of antibody-drug conjugates (ADCs). 7Ethanol-10NH2-11F-Camptothecin can inhibit tumor growth and is used in cancer research.
    7Ethanol-10NH2-11F-Camptothecin
  • HY-158391
    Anticancer agent 218
    		Inhibitor
    Anticancer agent 218 (P136) is a Camptothecin compound, with anticancer activity.
    Anticancer agent 218
  • HY-N4329
    Nidulalin A
    		Inhibitor
    Nidulalin A is a DNA topoisomerase II inhibitor with an IC50 of 2.2 μM. Nidulalin A has an IC50 of 172 μM for DNA topoisomerase I. Nidulalin A has certain cytotoxicity.
    Nidulalin A
  • HY-120185
    Saintopin
    		Inhibitor
    Saintopin is an antitumor antibiotic. Saintopin is also an inhibitor of DNA topoisomerases I and II. Saintopin induces DNA cleavage.
    Saintopin
  • HY-101647A
    Intoplicine dimesylate
    		Inhibitor 98.28%
    Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA.
    Intoplicine dimesylate
  • HY-10919
    C-1311
    		Inhibitor
    C-1311 shows to inhibit the catalytic activity of DNA topoisomerase II in vitro and in tumour cells. C-1311 prolongs G2 arrest followed by G2 to M transit and cell death during mitosis in the process of mitotic catastrophe.
    C-1311
  • HY-115991
    Topoisomerase IV inhibitor 2
    		Inhibitor
    Topoisomerase IV inhibitor 2 (compound 5d) is a potent DNA topoisomerase IV (TOPO IV) inhibitor with IC50s of 0.35 μM and 0.55 μM for TOPO IV and DNA gyrase, respectively. Topoisomerase IV inhibitor 2 has anti-bacterial activity, with MICs of 1.985 μM and 0.744 μM in Staphylococcus aureus Newman and Escherichia coli ATCC8739, respectively.
    Topoisomerase IV inhibitor 2
  • HY-158230
    SN-398
    		Inhibitor
    SN-398 is a derivative of Camptothecin (HY-158230), which is an antitumor drug. Acting by inhibiting mammalian DNA topoisomerase I (Topo I), stabilizing the Topo I-DNA complex prevents DNA rewiring to induce Topo I mediated DNA breaks. In Hela cell tests, SN-398 shows stronger antitumor activity than SN-38 (HY-13704) (IC50=1.562 μM). SN-398 can be used to study the anti-proliferation and growth inhibition of Topo I in cancer cells.
    SN-398
  • HY-146163
    Topoisomerase II inhibitor 7
    		Inhibitor
    Topoisomerase II inhibitor 7 (compound 3a) is a potent inhibitor of topoisomerase II alpha subtype, with an IC50 of 3.19 μM. Topoisomerase II inhibitor 7 can induce cell cycle arrest and apoptosis.
    Topoisomerase II inhibitor 7
  • HY-13551B
    Amsacrine (gluconate)
    		Inhibitor
    Amsacrine gluconate is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
    Amsacrine (gluconate)
  • HY-146497
    Topoisomerase I inhibitor 7
    		Inhibitor
    Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants. Topoisomerase I inhibitor 7 indicates prospects for further search of new antitumor agent candidates among the heteroarene-fused anthraquinones.
    Topoisomerase I inhibitor 7
  • HY-159483
    SelB-1
    		Inhibitor
    SelB-1 serves as a dual inhibitor for Topoisomerase I/II. SelB-1 possesses anticancer activity and can be utilized in the research of prostate cancer and colon cancer. Furthermore, SelB-1 is also capable of inducing autophagy gene expression and lipid peroxidation, while simultaneously reducing the level of GSH.
    SelB-1
  • HY-19943
    TLC388
    		Inhibitor
    TLC388 is a novel camptothecin analog with limited antitumor activity in metastatic NEC.
    TLC388
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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