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-171684
    Anti-CCL2 (Carlumab)-MC-Vc-PAB-SN38
    		Inhibitor
    Anti-CCL2 (Carlumab)-MC-Vc-PAB-SN38 is an antibody-drug conjugate (ADC) consisting of the humanized anti-CCL2 (chemokine ligand 2) antibody Carlumab (HY-P99188) conjugated to the linker Mc-VC-PAB and the topoisomerase I inhibitor SN38 (HY-13704). The ADC toxic molecule and linker part are Mc-VC-PAB-SN38 (HY-131057). Anti-CCL2 (Carlumab)-MC-Vc-PAB-SN38 can be used in cancer research.
    Anti-CCL2 (Carlumab)-MC-Vc-PAB-SN38
  • HY-177548
    Fmoc-Val-Cit-PAB-Exatecan
    		Inhibitor
    Fmoc-Val-Cit-PAB-Exatecan is a precursor form of Exatecan (HY-13631). Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
    Fmoc-Val-Cit-PAB-Exatecan
  • HY-170557
    Topoisomerase IIα-IN-10
    		Inhibitor
    Topoisomerase IIα-IN-10 (Compound 13r) is an inhibitor of Topoisomerase IIα. It binds to the active site of DNA when complexed with Topoisomerase IIα, and this binding is stabilized through interactions with DNA base pairs and amino acid residues. Topoisomerase IIα-IN-10 can induce Apoptosis by intercalating DNA and inhibiting Topoisomerase IIα, thereby disrupting the mitochondrial membrane potential and inhibiting the growth of HCT116 cell lines, with an IC50 of 4.37 μM against HCT116 cells. Topoisomerase IIα-IN-10 can be used for research in the field of cancer treatment.
    Topoisomerase IIα-IN-10
  • HY-117688
    WJ35435
    		Inhibitor
    WJ35435 is a dual-targeted anticancer hybrid that induces anti-HDAC (in particular HDAC1 and HDAC6) and anti-topoisomerase I activities that causes DNA damage associated with a low DNA repair capability and induces cell cycle arrest at G1- and G2-phase to apoptosis. WJ35435 induces histone H3 acetylation and phosphorylation, α-tubulin acetylation and γ-H2AX formation to achieve anti-HDAC effect. WJ35435 is promising for research of cancer.
    WJ35435
  • HY-N15597
    Melicopidine
    		Inhibitor
    Melicopidine (NSC 34757) is a DNA topoisomerase inhibitor, which is an acridone alkaloid found in the bark of Medicosma subsessilis. Melicopidine exerts potential antitumor activity by binding to DNA or inhibiting related enzyme activity.
    Melicopidine
  • HY-114668A
    Camptothecin-20(S)-O-propionate hydrate
    		Inhibitor
    Camptothecin-20(S)-O-propionate (Camptothecin-20-O-propionate) hydrate, the C20-propionate ester of CPT, is a highly effective anticancer agent. Camptothecin-20(S)-O-propionate hydrate is a topoisomerase-Ι inhibitor.
    Camptothecin-20(S)-O-propionate hydrate
  • HY-126142
    Top1 inhibitor 1
    		Inhibitor 99.67%
    Top1 inhibitor 1 (compound 28) is a potent human topoisomerase I (Top1) inhibitor with an IC50 value of 29 nM.
    Top1 inhibitor 1
  • HY-120638
    BMS-250749
    		Inhibitor
    BMS-250749 is a topoisomerase I (Top I) inhibitor of the fluoroglycosyl-3,9-difluoroindolecarbazole class. BMS-250749 exhibits potent cytotoxicity and selectivity, and shows curative antitumor activity against Lewis lung cancer. BMS-250749 exhibits broad-spectrum antitumor activity superior to CPT-11 in certain preclinical xenograft models..
    BMS-250749
  • HY-116926
    Deoxynybomycin
    		Inhibitor
    Deoxynybomycin is an antibiotic, that can be isolated from Streptomyces, and antibacterial activity against Staphylococcus aureus. Deoxynybomycin is the inhibitor for DNA gyrase and Topoisomerase I. Deoxynybomycin induces expression of p21/WAF1, exhibits cytotoxicity and induces apoptosis in cancer cells Saos-2, TMK-1, and THP-1.
    Deoxynybomycin
  • HY-103399R
    Trovafloxacin mesylate (Standard)
    		Inhibitor
    Clarithromycin (Standard) is the analytical standard of Clarithromycin. This product is intended for research and analytical applications. Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM. Clarithromycin significantly inhibits the HERG potassium current.Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K.
    Trovafloxacin mesylate (Standard)
  • HY-147839
    Topoisomerase II inhibitor 10
    		Inhibitor
    Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells.
    Topoisomerase II inhibitor 10
  • HY-179018
    Topoisomerase II-IN-25
    		Inhibitor
    Topoisomerase II-IN-25 (Compound 6a) is a selective inhibitor of topoisomerase II and has no inhibitory activity on topoisomerase I. Topoisomerase II-IN-25 exhibits significant anti-PC-3 cell activity. Topoisomerase II-IN-25 significantly increases intracellular ROS levels, inducing oxidative stress. Topoisomerase II-IN-25 causes depolarization of mitochondrial membrane potential and promotes cell apoptosis. Topoisomerase II-IN-25 blocks PC-3 cells in the G2/M phase. Topoisomerase II-IN-25 can be used for the study of prostate cancer.
    Topoisomerase II-IN-25
  • HY-W715630
    Salvicine
    		Inhibitor
    Salvicine is a DNA topoisomerase II inhibitor (IC50=3 μM). Salvicine increases the interaction between DNA and Topo II by interacting with the ATPase domain, inhibiting DNA degradation and ATP hydrolysis. Salvicine has anticancer activities, including inhibiting Topo II, causing DNA damage, overcoming multidrug resistance, and inhibiting tumor cell adhesion.
    Salvicine
  • HY-175272
    DBCO-PEG8-VKG-CPT2
    		Inhibitor
    DBCO-PEG8-VKG-CPT2 is a drug-linker conjugate for ADC. DBCO-PEG8-VKG-CPT2 consists of a topoisomerase 1 inhibitor (7-MAD-MDCPT) (HY-132162) and a stable and cleavable linker (DBCO-PEG8-VKG) (HY-175426). DBCO-PEG8-VKG-CPT2 can be used for synthesis of ADCs.
    DBCO-PEG8-VKG-CPT2
  • HY-115990
    Topoisomerase IV inhibitor 1
    		Inhibitor
    Topoisomerase IV inhibitor 2 (compound 7d) is a potent DNA topoisomerase IV (TOPO IV) inhibitor with IC50s of 0.23 μM and 0.43 μM for TOPO IV and DNA gyrase, respectively. Topoisomerase IV inhibitor 2 has anti-bacterial activity, with MICs of 0.972 μM and 0.608 μM in Staphylococcus aureus Newman and Escherichia coli ATCC8739, respectively.
    Topoisomerase IV inhibitor 1
  • HY-N8248A
    (-)-Eleutherin
    (-)-Eleutherin is a pyranonaphthoquinone derivative that exhibits cytotoxic activity by inhibiting DNA topoisomerase II. (-)-Eleutherin has been shown to have promising potential as a medicinal compound due to its association with naphthoquinones. (-)-Eleutherin demonstrates significant DNA fragmentation rates, indicating its strong cytotoxic effects on cells. Additionally, (-)-Eleutherin possesses higher antioxidant potential compared to control samples, contributing to its therapeutic efficacy.
    (-)-Eleutherin
  • HY-W046353R
    2-Methoxycinnamaldehyde (Standard)
    		Inhibitor
    2-Methoxycinnamaldehyde (Standard) is the analytical standard of 2-Methoxycinnamaldehyde. This product is intended for research and analytical applications. 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 (Standard)
  • HY-W040298
    Ciprofloxacin lactate
    		Inhibitor
    Ciprofloxacin (Bay-09867) lactate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin lactate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin lactate has anti-proliferative activity and induces apoptosis. Ciprofloxacin lactate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
    Ciprofloxacin lactate
  • HY-160598
    Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol
    		Inhibitor
    Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol (compound 45) is a camptothecin compound that can inhibit cell proliferation, with an IC50 of 2.92 ng/mL for MDA‑MB‑468 cells. Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol can be used for the research of cancer.
    Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol
  • HY-158390
    Anticancer agent 217
    		Inhibitor
    Anticancer agent 217 (35B) is a Camptothecin compound, with IC50 values of 6.2 nM and 7.1 nM in MCF-7 cells and MDA-MB-231 cells, respectively.
    Anticancer agent 217
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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