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-13622A
    Elomotecan
    		Inhibitor
    Elomotecan (BN 80927 free base) is a potent inhibitor of topoisomerases I and II. Elomotecan is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan reduces the proliferation of different tumor cells with higher potency than other anticancer agents of reference targeting topoisomerases I and II.
    Elomotecan
  • HY-13502AS
    Mitoxantrone-d8 dihydrochloride
    		Inhibitor
    Mitoxantrone-d8 dihydrochloride is deuterated labeled Mitoxantrone dihydrochloride (HY-13502A). Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity. Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.
    Mitoxantrone-d<sub>8</sub> dihydrochloride
  • HY-161095
    iRGD-CPT
    		Inhibitor
    iRGD-CPT is a conjugate of iRGD and camptothecin that is covalently coupled through a heterobifunctional linker. iRGD-CPT has anticancer activity in vitroandin vivo. iRGD-CPT can be used for the study of colon cancer.
    iRGD-CPT
  • HY-146227
    DNA topoisomerase II inhibitor 1
    		Inhibitor
    DNA topoisomerase II inhibitor 1 (compound 8ed) is a potent DNA topoisomerase II inhibitor. DNA topoisomerase II inhibitor 1 shows anti-proliferative activity. DNA topoisomerase II inhibitor 1 induces apoptosis and cell cycle arrest at sub G1 phase.
    DNA topoisomerase II inhibitor 1
  • HY-143281
    Topoisomerase II inhibitor 5
    		Inhibitor
    Topoisomerase II inhibitor 5 (Compound E24) is a DNA topoisomerase II inhibitor with anticancer activities.
    Topoisomerase II inhibitor 5
  • HY-155034
    Antitumor agent-102
    		Inhibitor
    Antitumor agent-102 (compound 10) is a conjugate of Topoisomerase I inhibitor SN38 and glucose transporter inhibitor, targeting to colorectal cancer. Antitumor agent-102 induces higher concentrations of free SN38 in tumor tissues than Irinotecan (HY-16562).
    Antitumor agent-102
  • HY-B0356AR
    Ciprofloxacin (monohydrochloride) (Standard)
    		Inhibitor
    Ciprofloxacin (monohydrochloride) (Standard) is the analytical standard of Ciprofloxacin (monohydrochloride). This product is intended for research and analytical applications. Ciprofloxacin (Bay-09867) monohydrochloride is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin monohydrochloride induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin monohydrochloride has anti-proliferative activity and induces apoptosis. Ciprofloxacin monohydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity[4].
    Ciprofloxacin (monohydrochloride) (Standard)
  • HY-168285
    LE01
    		Inhibitor
    LE01 is a drug-linker conjugate for ADC. LE01 contains a ADC linker and a DNA topoisomerase I inhibitor DXd (HY-13631D). LE01 can be used to synthesize HER2-targeting ADC (HER2-LE01).
    LE01
  • HY-146228
    HSP90-IN-13
    		Inhibitor
    HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway.
    HSP90-IN-13
  • HY-143265
    Topoisomerase I inhibitor 2
    		Inhibitor
    Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect.
    Topoisomerase I inhibitor 2
  • HY-161957
    Top1/2-IN-1
    		Inhibitor
    Top1/2-IN-1 (compound 23) is an orally available dual inhibitor of Top1/2 with antiproliferative activity. Top1/2-IN-1 damages DNA with increased levels of reactive oxygen species, inducing apoptosis and cell cycle arrest in cancer cells. Top1/2-IN-1 exhibits in vivo antitumor activity in xenograft models.
    Top1/2-IN-1
  • HY-14833
    Atiratecan
    		Inhibitor
    Atiratecan (TP300) is a proagent of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models.
    Atiratecan
  • HY-162805
    iNOS/TopoI-IN-1
    		Inhibitor
    iNOS/TopoI-IN-1 (compound AuL9) is a multi-target hybrid molecule with anti-tumor, anti-inflammatory and antioxidant activities. iNOS/TopoI-IN-1 inhibits the growth of breast cancer cells MCF-7 and MDA MB-231 in vitro with IC50 of 3.5 μM and 6.3 μM, respectively, and induces DNA damage and apoptosis of breast cancer cells by inhibiting human topoisomerase I (TopoI) (Ki=2.72 μM). In addition, NOS/TopoI-IN-1 inhibits the expression of iNOS by inhibiting the activation of NF-kB (Ki=1.49 μM).
    iNOS/TopoI-IN-1
  • 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-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
    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)
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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