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-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-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
  • HY-173625
    P5(PEG12)-VC-PAB-Exatecan
    		Inhibitor
    P5(PEG12)-VC-PAB-Exatecan (LP3) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker P5(PEG24)-VC-PAB to make antibody agent conjugate (ADC). P5(PEG12)-VC-PAB-Exatecan can be used for the research of tumor.
    P5(PEG12)-VC-PAB-Exatecan
  • HY-149348
    DiPT-4
    		Inhibitor
    DiPT-4 is a dual TOP1/PARP1 inhibitor that induces massive DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells. DiPT-4 has the potential to overcome cancer drug resistance.
    DiPT-4
  • HY-13725R
    Pirarubicin (Standard)
    		Inhibitor
    Pirarubicin (Standard) is the analytical standard of Pirarubicin. This product is intended for research and analytical applications. Pirarubicin is an anthracycline antibiotics, acts as a topoisomerase II inhibitor, and is a widely used for treatment of various cancers, in particular, solid tumors.
    Pirarubicin (Standard)
  • HY-10529R
    Betulinic acid (Standard)
    		Inhibitor
    Betulinic acid (Standard) is the analytical standard of Betulinic acid. This product is intended for research and analytical applications. Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties.
    Betulinic acid (Standard)
  • HY-49861
    Exatecan intermediate 11
    		Inhibitor
    Exatecan intermediate 11 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM).
    Exatecan intermediate 11
  • HY-101064S4
    Fmoc-leucine-15N
    		Inhibitor
    Fmoc-leucine-15N is a 15N-labeled and 13C-labled EIDD-1931. EIDD-1931 (Beta-d-N4-hydroxycytidine; NHC) is a novel nucleoside analog and behaves as a potent anti-virus agent. EIDD-1931 effectively inhibits the replication activity of venezuelan equine ence
    Fmoc-leucine-<sup>15</sup>N
  • HY-114684
    A20832
    		Inhibitor
    A20832 is a specific resolvase inhibitor that blocks both the recombination and topoisomerase activities of resolvase. A20832 inhibits the site-specific recombination reaction mediated by the Tn3-encoded resolvase protein at the strand cleavage step and has no effect on synapsis.
    A20832
  • HY-N6054R
    Niranthin (Standard)
    		Inhibitor
    Niranthin (Standard) is the analytical standard of Niranthin. This product is intended for research and analytical applications. Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
    Niranthin (Standard)
  • HY-156464
    Topoisomerase I inhibitor 10
    		Inhibitor
    Topoisomerase I inhibitor 10 (compound 13) is a leishmanial topoisomerase IB inhibitor. Topoisomerase I inhibitor 10 has antileishmanial activity against L. donovani promastigotes, with the IC50 of 27.91 μM.
    Topoisomerase I inhibitor 10
  • HY-10581B
    Gatifloxacin mesylate
    		Inhibitor
    Gatifloxacin mesylate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin mesylate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin mesylate can be used to treat bacterial conjunctivitis in vivo.
    Gatifloxacin mesylate
  • HY-W781148
    Suptopin-2
    		Inhibitor
    Sutopin-2 is a topoisomerase II inhibitor. Suptopin-2 affects cell cycle progression and stability of microtubules. Sutopin-2 induces cell cycle arrest by regulating the nucleocytoplasmic transport of cyclin B1.
    Suptopin-2
  • HY-167671
    BE-10988
    		Inhibitor
    BE-10988 is a DNA topoisomerase inhibitor. BE-10988 inhibits the growth of Doxorubicin (HY-15142A)-resistant and vincristine-resistant P388 mouse leukemia cell lines by increasing the formation of DNA topoisomerase complexes.
    BE-10988
  • HY-B0395D
    (1R,2S,7R)-Sitafloxacin
    		Inhibitor
    (R)-Sitafloxacin (DU-6857), a stereoisomer of Sitafloxacin (DU-6859a), is also an inhibitor of topoisomerases, with an IC50 of 0.18 μg/mL of DNA gyrase.
    (1R,2S,7R)-Sitafloxacin
  • HY-10581AS1
    Gatifloxacin-d4 hydrochloride
    		Inhibitor
    Gatifloxacin-d4 (AM-1155-d4; BMS-206584-d4; PD135432-d4) hydrochloride is deuterium-labeled Gatifloxacin (hydrochloride) (HY-10581A).
    Gatifloxacin-d<sub>4</sub> hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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