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-135867E
    NHC-triphosphate tetraammonium
    		Inhibitor
    NHC-triphosphate tetraammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a triphosphate form. NHC-triphosphate tetraammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA.
    NHC-triphosphate tetraammonium
  • HY-118581
    Coralyne chloride
    		Inhibitor 98.39%
    Coralyne chloride is a protoberberine alkaloid with potent anti-cancer activities. Coralyne chloride acts as a potent topoisomerase I poison and induces Top I mediated DNA cleavage. Coralyne chloride can be used for preparing?coralyne derivatives?as DNA binding fluorescent probes.
    Coralyne chloride
  • HY-174374
    Topobexin
    		Inhibitor 99.04%
    Topobexin is a TOP2B-selective inhibitor with IC50 values of 0.19 μM and 4.8 μM for TOP2B and TOP2A (DNA decatenation assay). Topobexin binds to non-homologous residues in the obex pocket and targets the ATPase domain of TOP2B. Topobexin prevents anthracycline-induced DNA double-strand break formation, apoptotic signaling mediated by caspase 3/7, 8 and 9, cardiomyocyte morphological changes, mitochondrial depolarization/loss, left ventricular systolic dysfunction, extracellular matrix remodeling, fibrotic alterations, and increases in plasma cardiac troponin T and BNP. Topobexin does not impair the antiproliferative effects of anthracyclines in cancer cells, exhibits no intrinsic cytotoxicity in cardiomyocytes, and is well tolerated in rabbits. Topobexin can be used in studies related to anthracycline-induced cardiotoxicity.
    Topobexin
  • HY-B0398A
    Nalidixic acid sodium salt
    		Inhibitor 99.83%
    Nalidixic acid sodium salt, a quinolone antibiotic, is effective against both gram-positive and gram-negative bacteria. Nalidixic acid acts in a bacteriostatic manner in lower concentrations and is bactericidal in higher concentrations. Nalidixic acid inhibits a subunit of DNA gyrase and topoisomerase IV and reversibly blocks DNA replication in susceptible bacteria.
    Nalidixic acid sodium salt
  • HY-100309
    9-Aminocamptothecin
    		Inhibitor 98.89%
    9-Aminocamptothecin (9-Amino-CPT) is a topoisomerase I inhibitor with potent anticancer activity.
    9-Aminocamptothecin
  • HY-13758A
    TAS-103 dihydrochloride
    		Inhibitor 98.45%
    TAS-103 dihydrochloride is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
    TAS-103 dihydrochloride
  • HY-153031
    Val-Cit-PAB-Exatecan
    		Inhibitor 99.79%
    Val-Cit-PAB-Exatecan (Val-Cit-PAB-DX8951) is a agent-linker conjugate for ADC. Val-Cit-PAB-Exatecan is composed of a DNA topoisomerase I DX-8951 (HY-13631) and a cathepsin cleavable ADC linker.
    Val-Cit-PAB-Exatecan
  • HY-173634
    Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan
    		Inhibitor 99.95%
    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-13551A
    Amsacrine hydrochloride
    		Inhibitor 99.92%
    Amsacrine hydrochloride (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
    Amsacrine hydrochloride
  • HY-163099
    P5(PEG24)-VC-PAB-Exatecan
    		Inhibitor 99.74%
    P5 (PEG24)-VC-PAB-Exatecan is a TOP1 inhibitor payload with antibody-conjugation-dependent activity. Conjugation of P5 (PEG24)-VC-PAB-Exatecan with Trastuzumab (HY-P9907) generates a DAR8 antibody-drug conjugate (ADCs) with antibody-like pharmacokinetic properties. P5 (PEG24)-VC-PAB-Exatecan induces S-phase and G2-M-phase cell cycle arrest, DNA damage and apoptosis in target-positive tumor cells, and releases damage-associated molecular patterns (DAMP) related to immunogenic cell death (ICD). The ADCs prepared from it exert bystander killing effects on non-target tumor cells. ADCs based on P5 (PEG24)-VC-PAB-Exatecan exhibit linker stability in vitro and in vivo, show in vivo efficacy, and can be used in research related to HER2-positive cancers.
    P5(PEG24)-VC-PAB-Exatecan
  • HY-16518
    Voreloxin Hydrochloride
    		Inhibitor 99.73%
    Voreloxin Hydrochloride is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.
    Voreloxin Hydrochloride
  • HY-13061
    Daun02
    		Inhibitor 98.72%
    Daun02 is a proagent of the topoisomerase inhibitor Daunorubicin.
    Daun02
  • HY-13744
    Rubitecan
    		Inhibitor 99.41%
    Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells.
    Rubitecan
  • HY-16261B
    MC-DOXHZN hydrochloride
    		Inhibitor 98.0%
    MC-DOXHZN ((E/Z)-Aldoxorubicin; Doxorubicin(6-maleimidocaproyl)hydrazone) hydrochloride is an albumin-binding proagent of Doxorubicin (HY-15142A) (DNA topoisomerase II inhibitor), with acid-sensitive properties. MC-DOXHZN hydrochloride can be used to synthesize ADC.
    MC-DOXHZN hydrochloride
  • HY-18351
    Indotecan
    		Inhibitor 98.0%
    Indotecan (LMP-400), an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis.
    Indotecan
  • HY-B0067
    Amrubicin
    		Inhibitor ≥98.0%
    Amrubicin (SM-5887) is a DNA topoisomerase II inhibitor, used for the research of cancer.
    Amrubicin
  • HY-N0311
    Emodin-8-glucoside
    		Inhibitor 99.35%
    Emodin-8-glucoside is an anthraquinone derivative that can be isolated from Aloe vera. Emodin-8-glucoside is the inhibitor for MAPK with an inhibition constant of 430.14 pM. Emodin-8-glucoside exhibits moderate inhibitory activity against rat lens aldose reductase (ALAR) and topoisomerases II with IC50s of 14.4 μM and 66 μM. Emodin-8-glucoside exhibits antioxidant, anti-inflammatory and anti-fibrotic activities. Emodin-8-glucoside can cross the blood brain barrier.
    Emodin-8-glucoside
  • HY-N2108
    7-Ethylcamptothecin
    		Inhibitor 99.58%
    7-Ethylcamptothecin is a derivative of Camptothecin (HY-16560) and a DNA topoisomerase I inhibitor that exhibits significant antitumor activity against tumor cells. 7-Ethylcamptothecin serves as a key precursor for the synthesis of 20 (S)-O-substituted benzoyl-7-ethylcamptothecin compounds. 7-Ethylcamptothecin is widely used in various tumor-related scientific studies.
    7-Ethylcamptothecin
  • HY-N6714
    Alternariol
    		Inhibitor 99.88%
    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
  • HY-W046353
    2-Methoxycinnamaldehyde
    		Inhibitor 98.95%
    2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound that can be isolated from Cinnamomum cassia. 2-Methoxycinnamaldehyde inhibits topoisomerase-I/II and NF-κB signaling pathway, causes mitochondrial dysfunction, induces lysosomal vesiculation, thereby leading to DNA damage and cell apoptosis. 2-Methoxycinnamaldehyde exhibits antitumor effects.
    2-Methoxycinnamaldehyde
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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