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-145852
    Top/HDAC-IN-2
    		Inhibitor
    Top/HDAC-IN-2 (45b), a Top and HDAC dual inhibitor, exhibits potent antitumor activities and induces apoptosis.
    Top/HDAC-IN-2
  • HY-149271
    Anti-MRSA agent 7
    		Inhibitor
    Anti-MRSA agent 7 (Compound 12) is a potent antibacterial agent. Anti-MRSA agent 7 inhibits S. aureus DNA gyrase, E. coli DNA gyrase, S. aureus topo IV and E. coli topo IV with IC50s of 0.185, 0.365, 0.341 and 0.059 μM, respectively.
    Anti-MRSA agent 7
  • HY-162380
    Topoisomerase II inhibitor 18
    		Inhibitor
    Topoisomerase II inhibitor 18 (Compound IV) is a Quinoxaline derivative, which inhibits topoisomerase II with IC50 of 7.5 μM. Topoisomerase II inhibitor 18 inhibits proliferation, cell cycle at S phase and induces apoptosis in PC-3 cells. Topoisomerase II inhibitor 18 reveals antitumor activity against cancer.
    Topoisomerase II inhibitor 18
  • HY-173634
    Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan
    		Inhibitor
    Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan (LP1) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB (HY-173635) to make antibody agent conjugate (ADC), AZD0516 (HY-173639).
    Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan
  • HY-168739
    Topoisomerase I inhibitor 17
    		Inhibitor
    Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice.
    Topoisomerase I inhibitor 17
  • HY-N0498R
    Nitidine chloride (Standard)
    		Inhibitor
    Nitidine (chloride) (Standard) is the analytical standard of Nitidine (chloride). This product is intended for research and analytical applications. Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.
    Nitidine chloride (Standard)
  • HY-143279
    Topoisomerase II inhibitor 3
    		Inhibitor
    Topoisomerase II inhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a Type II DNA topoisomerase (topo II) inhibitor , as a topo IIα/β inhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential.
    Topoisomerase II inhibitor 3
  • HY-116933
    Murrayanol
    		Inhibitor
    Murrayanol is a natural carbazole alkaloid with a variety of biological activities. Murrayanol shows anti-inflammatory, topoisomerase I and topoisomerase II (Topoisomerase) inhibition activities. Murrayanol also as a mosquitocidal and antimicrobial.
    Murrayanol
  • HY-13726
    Piroxantrone
    		Inhibitor
    Piroxantrone (Oxantrazole) is a potent DNA topoisomerase II-targeting anthrapyrazole antitumor agent. Piroxantrone displays cardiotoxicity.
    Piroxantrone
  • HY-146316
    Topoisomerase II inhibitor 6
    		Inhibitor
    Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective inhibitor of topoisomerase II. Topoisomerase II inhibitor 6 exhibits antiproliferative activity on different tumor cell lines. Topoisomerase II inhibitor 6 blocks the cell cycle of CCRF-CEM in the G2 phase and induces DNA DSB. Topoisomerase II inhibitor 6 has the potential for the research of cancer diseases.
    Topoisomerase II inhibitor 6
  • HY-10982A
    Amonafide dihydrochloride
    		Inhibitor
    Amonafide dihydrochloride (AS1413 dihydrochloride) is a topoisomerase II (Topo II) inhibitor and DNA intercalator with activity in inducing apoptotic signaling. Amonafide dihydrochloride can inhibit the binding of Topo II to DNA, thereby preventing the synthesis of DNA and RNA. Amonafide dihydrochloride maintains cytotoxic activity in the presence of P-glycoprotein-mediated multidrug resistance (MDR).
    Amonafide dihydrochloride
  • HY-149239
    Topo II/HDAC-IN-2
    		Inhibitor
    Topo II/HDAC-IN-2 (8d) exhibits excellent dual inhibitory activities against Topo II and HDAC. Topo II/HDAC-IN-2 (8d) induces apoptosis.
    Topo II/HDAC-IN-2
  • HY-17460B
    Garenoxacin mesylate
    		Inhibitor
    Garenoxacin (BMS 284756) mesylate is an orally active quinolone antibiotic and Garenoxacin mesylate has a broad spectrum of activity against a wide array of gram-positive and gram-negative bacteria, anaerobes. Garenoxacin mesylate also inhibits Gyrase and TOPO IV.
    Garenoxacin mesylate
  • HY-162341
    Topoisomerase I inhibitor 15
    		Inhibitor
    Topoisomerase I inhibitor 15 (compound 4b) is an inhibitor of topoisomerase I with anticancer activity. Topoisomerase I inhibitor 15 inhibits A549 cells with an IC50 of 7.34 μM.
    Topoisomerase I inhibitor 15
  • HY-144654
    HDAC/Top-IN-1
    		Inhibitor
    HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC50s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy.
    HDAC/Top-IN-1
  • HY-126054
    A1062
    		Inhibitor
    A1062 is an inhibitor for Tn3 encoded resolvase with IC50 in micromolar level. A1062 suppresses the binding of resolvase proteins to res sites, and blocks resolvase-induced site-specific recombination.
    A1062
  • HY-156969
    Topoisomerase I inhibitor 11
    		Inhibitor
    Topoisomerase I inhibitor 11 is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 11 can bind to BTK.
    Topoisomerase I inhibitor 11
  • HY-148719
    ARN24139
    		Inhibitor
    ARN24139(compound 3f) is a topoisomerase II (topoII) inhibitor with the IC50 of 7.3 μM. ARN24139 can inhibit cancer cell proliferation and is well tolerated in vivo.
    ARN24139
  • HY-158389
    Anticancer agent 216
    		Inhibitor
    Anticancer agent 216 (34A) is a Camptothecin compound, with IC50 values of 9.6 nM and 11.6 nM in MCF-7 cells and MDA-MB-231 cells, respectively.
    Anticancer agent 216
  • HY-13631AS1
    Exatecan-d3 mesylate
    		Inhibitor
    Exatecan-d3 (DX8951f-d3) mesylate is deuterium-labeled Exatecan mesylate (HY-13631A). Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL.
    Exatecan-d<sub>3</sub> mesylate
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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