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-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-N0311R
    Emodin-8-glucoside (Standard)
    		Inhibitor
    Emodin-8-glucoside (Standard) is the analytical standard of Emodin-8-glucoside. This product is intended for research and analytical applications. 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 (Standard)
  • HY-175834
    DNA/TOP2A-IN-1
    		Inhibitor
    DNA/TOP2A-IN-1 is an inhibitor of DNA and TOP2A. DNA/TOP2A-IN-1 selectively binds to TOP2A, not TOP2B, and interacts with DNA and TOP2A to form a stable DM1-TOP2A-DNA ternary complex. DNA/TOP2A-IN-1 induces DNA damage, increases reactive oxygen species (ROS) and triggers apoptosis in triple-negative breast cancer (TNBC) cells. DNA/TOP2A-IN-1 disrupts microtubule distribution and induces cell cycle arrest. DNA/TOP2A-IN-1 shows strong antiproliferative activity and inhibits cell migration. DNA/TOP2A-IN-1 inhibits tumor growth and can be used for TNBC research.
    DNA/TOP2A-IN-1
  • HY-W800535
    Cryptolepine
    		Inhibitor
    Cryptolepine is an orally active multi-potent alkaloid with anti-cancer, anti-bacterial, anti-viral, anti-malarial, anti-inflammatory, anti-hyperglycemic, relieve pain and other properties. Cryptolepine acts as an inhibitor of c-Myc, mTOR, NF-κB, HIF-1, MAPK and an activator of AMPKα1/2. It intercalates into DNA, inhibits topoisomerase II (Top II), disrupts mitochondrial dynamics and induces apoptosis. Cryptolepine also exhibits anti-plasmodial and cholinesterase inhibitory activities. Cryptolepine can be used in research related to tumors (melanoma, hepatocellular carcinoma, mammary adenocarcinoma, etc.), malaria, inflammatory diseases and diabetes, particularly in studies focused on inhibiting tumor growth and anti-plasmodial infection.
    Cryptolepine
  • 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-177686
    N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan)
    N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
    N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan)
  • 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-19211
    KW-2170 hydrochloride
    		Inhibitor
    KW-2170 hydrochloride is an alkylating agent and topoisomerase II inhibitor. KW-2170 hydrochloride stabilizes the topoisomerase II-DNA complex, causing DNA double-strand breaks, thereby preventing DNA replication and transcription, and ultimately leading to the death of tumor cells. KW-2170 hydrochloride exhibits potent and broad-spectrum anti-tumor activity in various mouse and human tumor models. KW-2170 hydrochloride can be used in the research of solid tumors.
    KW-2170 hydrochloride
  • HY-181725
    Topoisomerase I-IN-20
    		Inhibitor
    Topoisomerase I-IN-20 is a Topoisomerase I inhibitor. Topoisomerase I-IN-20 disrupts DNA synthesis and transcription, thereby inhibiting the proliferation and migration of cancer cells. Topoisomerase I-IN-20 induces S-phase cell cycle arrest and mitochondria-mediated Apoptosis in cancer cells, which is characterized by upregulated expression of p53, Bax, caspase-3 and caspase-9, along with downregulated expression of Bcl-2. Topoisomerase I-IN-20 increases intracellular ROS levels. Topoisomerase I-IN-20 is applicable to lung cancer-related research.
    Topoisomerase I-IN-20
  • 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-N8250
    cis-THSG
    		Inhibitor
    cis-THSG is a selective and orally active DNA topoisomerase II inhibitor with no activity against DNA topoisomerase I. cis-THSG suppresses transcription of PEPCK. cis-THSG reduces blood glucose levels, ameliorates glucose intolerance, and alleviates insulin resistance in high fat diet-induced diabetic male CF-1 mice. cis-THSG can be used for the research of type 2 diabetes mellitus.
    cis-THSG
  • HY-179616
    AT-9
    AT-9 is an anthraquinone-triazene derivative. AT-9 exhibits strong DNA intercalation ability. AT-9 can also interact with Topo IIA. AT-9 exhibits anticancer activity against non-small cell lung cancer and cervical cancer.
    AT-9
  • 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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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