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-N8473
    Pericosine A
    		Inhibitor
    Pericosine A ((+)-Pericosine A) is a topoisomerase II (Topoisomerase II) inhibitor that can be isolated from the Periconia byssoides strain. Pericosine A has significant antitumor activity in vitro and in vivo and can be used in cancer research. Pericosine A also inhibits the protein kinase epidermal growth factor receptor.
    Pericosine A
  • HY-153069A
    GGFG-PAB-Exatecan TFA
    		Inhibitor
    GGFG-PAB-Exatecan TFA consists of an ADC toxin Exatecan (HY-13631) and a linker GGFG-PAB, and can be used as a drug-linker conjugate for the synthesis of ADC molecules.
    GGFG-PAB-Exatecan TFA
  • HY-79490S
    Ac-Exatecan-d5
    		Inhibitor 99.93%
    Ac-Exatecan-d5 is the deuterium labeled Ac-Exatecan (HY-79490).
    Ac-Exatecan-d<sub>5</sub>
  • HY-161385
    Topoisomerase I inhibitor 16
    		Inhibitor
    Topoisomerase I inhibitor 21 (Compound 3e) is an inhibitor for Topoisomerase I through stabilization of enzyme-DNA complex. Topoisomerase I inhibitor 21 exhibits antiproliferative activity in 39 human cancer cells (JFCR39) with mean GI50 39 nM.
    Topoisomerase I inhibitor 16
  • HY-N6714R
    Alternariol (Standard)
    		Inhibitor
    Alternariol (Standard) is the analytical standard of Alternariol. This product is intended for research and analytical applications. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects.
    Alternariol (Standard)
  • HY-135845
    TP3011
    		Inhibitor
    TP3011 (CH0793011) is an active metabolite of CH-0793076 and is a potent topoisomerase I inhibitor equipotent as SN38. TP3011 is against cancer cell lines growth with IC50s at the range sub-nanomolar in vitro.
    TP3011
  • 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-W744739
    Betulinic acid-d3
    Betulinic acid-d3 (Lupatic acid-d3) is a deuterium labeled Betulinic acid (HY-10529). 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-d<sub>3</sub>
  • 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-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 15N-labled Fmoc-leucine (HY-101064).
    Fmoc-leucine-<sup>15</sup>N
  • HY-119425R
    Razoxane (Standard)
    		Inhibitor
    Razoxane (Standard) is the analytical standard of Razoxane. This product is intended for research and analytical applications. Razoxane (ICRF 159) is an antiangiogenic topoisomerase II inhibitor, can be used for the research of renal cell carcinoma (RCC).
    Razoxane (Standard)
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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