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-148819
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
    		Inhibitor 98.71%
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT (compound I) is a topoisomerase I inhibitor, which can be delivered to cells through conjugated antibody targeting, and has good ADC activity in vivo and in vitro.
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
  • HY-79490
    Ac-Exatecan
    		Inhibitor 99.02%
    Ac-Exatecan is acetylation-modified Exatecan (HY-13631). Exatecan is a common toxin component in ADC preparation (ADC cytotoxin) and an inhibitor of DNA topoisomerase I (IC50 = 2.2 μM). Exatecan has antitumor activity. Exatecan can be used as a payload for ADC. Exatecan is effective against P-glycoprotein mediated multi-drug resistant cells.
    Ac-Exatecan
  • HY-16261B
    MC-DOXHZN hydrochloride
    		Inhibitor 98.04%
    MC-DOXHZN ((E/Z)-Aldoxorubicin) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), with acid-sensitive properties.
    MC-DOXHZN hydrochloride
  • 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-16518
    Voreloxin Hydrochloride
    		Inhibitor 99.58%
    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-17381A
    Idarubicin
    		Inhibitor 99.89%
    Idarubicin is an orally active and potent anthracycline antileukemic agent. Idarubicin inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription. Idarubicin shows induction of DNA damage. Idarubicin inhibits DNA synthesis and of c-myc expression. Idarubicin inhibits the growth of bacteria and yeasts.
    Idarubicin
  • HY-13721
    Phenoxodiol
    		Inhibitor 99.89%
    Phenoxodiol (Idronoxil), a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner.
    Phenoxodiol
  • 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-100309
    9-Aminocamptothecin
    		Inhibitor 98.89%
    9-Aminocamptothecin (9-Amino-CPT) is a topoisomerase I inhibitor with potent anticancer activity.
    9-Aminocamptothecin
  • 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-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-163099
    P5(PEG24)-VC-PAB-Exatecan
    		Inhibitor 99.74%
    P5(PEG24)-VC-PAB-Exatecan (LP5) 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(PEG24)-VC-PAB-Exatecan can be used for the research of tumor.
    P5(PEG24)-VC-PAB-Exatecan
  • HY-W010800A
    Cholesterol hemisuccinate Tris salt
    		Inhibitor 98.0%
    Cholesterol hemisuccinate Tris salt (CHS-Tris) is a with hepatoprotective an anticancer activity. Cholesterol hemisuccinate Tris salt inhibits Acetaminophen (AAP, HY-66005) hepatotoxicity, and prevents AAP-induced hepatic apoptosis and necrosis. Cholesterol hemisuccinate Tris salt inhibits DNA polymerase and DNA topoisomerase to inhibit DNA replication and repair and cell division. Thus, Cholesterol hemisuccinate Tris salt inhibits tumor growth.
    Cholesterol hemisuccinate Tris salt
  • HY-B0330R
    Levofloxacin (Standard)
    		Inhibitor
    Levofloxacin (Standard) is the analytical standard of Levofloxacin. This product is intended for research and analytical applications. Levofloxacin ((-)-Ofloxacin) is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin inhibits the DNA gyrase and topoisomerase IV. Levofloxacin can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin shows anti-orthopoxvirus activity.
    Levofloxacin (Standard)
  • 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-156617A
    (αR)-Cyclopropaneacetamide-Exatecan
    		Inhibitor 99.93%
    (αR)-Cyclopropaneacetamide-Exatecan (compound 2-A), an Exenotecan derivative, is a cytotoxic agent. (αR)-Cyclopropaneacetamide-Exatecan inhibits U87MG and SK-BR-3 cells proliferation, with IC50s of 8.11 and 2.31 μM.
    (αR)-Cyclopropaneacetamide-Exatecan
  • 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-12930
    SPR719
    		Inhibitor 99.39%
    SPR719 (VXc-486) is an orally active gyrase B inhibitor, with bactericidal activity. SPR719 potently inhibits multiple agent-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis, with MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively. SPR719 is promising for research of lung disease caused by non-tuberculous mycobacteria (NTM).
    SPR719
  • HY-B0067
    Amrubicin
    		Inhibitor ≥98.0%
    Amrubicin (SM-5887) is a DNA topoisomerase II inhibitor, used for the research of cancer.
    Amrubicin
  • HY-13061
    Daun02
    		Inhibitor 98.72%
    Daun02 is a proagent of the topoisomerase inhibitor Daunorubicin.
    Daun02
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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