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-178373
    Topoisomerase I-IN-18
    		Inhibitor
    Topoisomerase I-IN-18, a derivative of Thiosemicarbazide (HY-Y0032), is a Topoisomerase I inhibitor. Topoisomerase I-IN-18 can disrupt DNA synthesis and transcription. Topoisomerase I-IN-18 inhibits tumor cell proliferation by inducing S-phase cell cycle arrest. Topoisomerase I-IN-18 can enhance mitochondria-mediated apoptosis, suppress cell migration, and increase intracellular Reactive Oxygen Species (ROS) levels. Topoisomerase I-IN-18 can increase p53 protein expression, γH2AX phosphorylation, upregulate Bax expression, downregulate Bcl-2 expression, and activate the caspase cascade. Topoisomerase I-IN-18 can be used for the study of lung cancer.
    Topoisomerase I-IN-18
  • HY-N2062
    10-Nitrocamptothecin
    		Inhibitor
    10-Nitrocamptothecin is a topoisomerase I inhibitor with an IC50 of 0.64 μM. 10-Nitrocamptothecin interferes with the formation of cleavable complexes, thereby inhibiting the activity of Topoisomerase I. 10-Nitrocamptothecin is applicable for cancer research.
    10-Nitrocamptothecin
  • HY-161970
    XSJ05
    		Inhibitor
    XSJ05 is a camptothecin (CPT) derivative that can inhibit topoisomerase I (Topo I) to exert anti-cancer activity. XSJ05 can trigger DNA double-strand breaks, leading to DNA damage. XSJ05 can inhibit the growth of colorectal cancer (CRC), arrest the cell cycle in G2/M phase, and induce apoptosis.
    XSJ05
  • HY-123143
    XR11576
    		Inhibitor
    XR11576 (MLN576) is an orally active inhibitor of topoisomerase I and II. XR11576 shows cytotoxicity against human and murine tumor cell lines (IC50: 6-47 nM).
    XR11576
  • HY-167671
    BE-10988
    		Inhibitor
    BE-10988 is a DNA topoisomerase inhibitor. BE-10988 inhibits the growth of Doxorubicin (HY-15142A)-resistant and vincristine-resistant P388 mouse leukemia cell lines by increasing the formation of DNA topoisomerase complexes.
    BE-10988
  • HY-159966
    Top/HDAC-IN-3
    		Inhibitor
    Top/HDAC-IN-3 (Compound 31) is an orally active dual inhibitor of Topoisomerase and HDAC. Top/HDAC-IN-3 increases reactive oxygen species (ROS) levels, leading to DNA damage, thereby inhibiting cancer cell colony formation and migration, inducing cancer cell Apoptosis, and causing cell cycle arrest. In the NSCLC model, Top/HDAC-IN-3 exhibited significant antitumor effects, with a tumor growth inhibition (TGI) of 77.5% at 100 mg/kg, surpassing the efficacy of the HDAC inhibitor SAHA (HY-10221) and the combination of SAHA (HY-10221) with the topoisomerase inhibitor Irinotecan (HY-16562).
    Top/HDAC-IN-3
  • HY-147801
    Topoisomerase IIα-IN-3
    		Inhibitor
    Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cell cycle at the G0/G1 phase and induces apoptosis.
    Topoisomerase IIα-IN-3
  • HY-149002
    Topoisomerase I/II inhibitor 4
    		Inhibitor
    Topoisomerase I/II inhibitor 4 (compound F16) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 4 inhibits cell proliferation, invasion and migration and induces apoptosis. Topoisomerase I/II inhibitor 4 can be used for liver cancer research.
    Topoisomerase I/II inhibitor 4
  • HY-131438
    GI-149893
    		Inhibitor
    GI-149893 is a selective topoisomerase I (TopoI) inhibitor. GI-149893 prevents DNA religation and induces irreversible DNA damage in tumor cells. GI-149893 is promising for research of cancers (e.g., colon carcinoma HT-29/SW-48, breast MX-1, prostate PC-3 xenografts).
    GI-149893
  • HY-109113
    Camsirubicin
    		Inhibitor
    Camsirubicin (GPX-150) is a non-cardiotoxic Doxorubicin (HY-15142) analog that selectively targets topoisomerase IIβ. Camsirubicin reduces cell viability and clone formation of MDA-MB-468 breast cancer cells. Camsirubicin increases the exposure of CALR and HSP90 on the cell surface. Camsirubicin can be used for the study of breast cancer.
    Camsirubicin
  • HY-120679A
    XK469 sodium
    		Inhibitor
    XK469 (NSC 697887) sodium is a quinoxaline-based topoisomerase II inhibitor. XK469 sodium exhibits antiproliferative activity against neuroblastoma cells. XK469 sodium can be used in the research of neuroblastoma.
    XK469 sodium
  • HY-186185
    OSu-Val-Cit-PAB-Exa
    		Inhibitor
    OSu-Val-Cit-PAB-Exa (compound D) is a cleavable linker-payload conjugate (usable for ADC synthesis). OSu-Val-Cit-PAB-Exa bears an N-terminal N-hydroxysuccinimide (OSu) ester group, and comprises Val-Cit, p-aminobenzyl alcohol (PAB) and Exatecan (HY-13631). OSu-Val-Cit-PAB-Exa serves as a payload-linker intermediate for polypeptide conjugation.
    OSu-Val-Cit-PAB-Exa
  • HY-148380
    Mal-PEG8-Phe-Lys-PAB-Exatecan
    		Inhibitor
    Mal-PEG8-Phe-Lys-PAB-Exatecan (compound 15) is a agent-linker conjugate for ADC, composed of degradable linker Mal-PEG8-Phe-Lys-PAB and toxin molecule Exatecan (HY-13631) composition.
    Mal-PEG8-Phe-Lys-PAB-Exatecan
  • HY-168848
    KT32
    		Inhibitor
    KT32 (10c) is a potent dual inhibitor of HDAC and Topo II α. KT32 induces cell death through apoptosis.
    KT32
  • HY-181018
    Topo I/DDX5-IN-1
    		Inhibitor
    Topo I/DDX5-IN-1 (Compound A10) is a Topo I and DDX5 inhibitor. Topo I/DDX5-IN-1 inhibits Topo I activity, binds to DDX5, and suppresses DDX5 function. Topo I/DDX5-IN-1 increases expression of γ-H2AX and p21, suppresses the expression of antiapoptotic proteins (Bcl-2 and XIAP), stimulates ROS generation, and triggers Apoptosis. Topo I/DDX5-IN-1 exhibits anticancer activity against pancreatic cancer, non-small cell lung cancer, skin cancer, and colorectal cancer.
    Topo I/DDX5-IN-1
  • HY-17460AR
    Garenoxacin Mesylate hydrate (Standard)
    		Inhibitor
    ACHE-IN-38 (hydrochloride) (Standard) is the analytical standard of ACHE-IN-38 (hydrochloride). This product is intended for research and analytical applications. ACHE-IN-38 hydrochloride (Compound 13b) inhibits the metabolic breakdown of the neurotransmitter acetylcholine (ACh) by the enzyme acetylcholinesterase (AChE) and hence alleviates memory deficits in patients with Alzheimer’s Disease by potentiating cholinergic transmission.
    Garenoxacin Mesylate hydrate (Standard)
  • HY-178315
    Exatecan analog 38
    		Inhibitor
    Exatecan analog 38 is a camptothecin derivative with potent topoisomerase I inhibitory activity. Exatecan analog 38 can be connected to monoclonal antibodies via linkers to form antibody-drug conjugate (ADC) molecules. Exatecan analog 38 can be used for cancer research.
    Exatecan analog 38
  • HY-184245
    Hsp90-IN-48
    		Inhibitor
    Hsp90-IN-48 is an orally active Hsp90 inhibitor with an IC50 of 19.4 nM. Hsp90-IN-48 improves tumor-cell uptake and intracellular active-component release, and suppresses tumor metastasis. Hsp90-IN-48 induces G2/M phase cell cycle arrest and tumor cell apoptosis whlie simultaneously inhibits Top1/Top2 activity. Hsp90-IN-48 inhibits tumor growth and can be used for colon cancer research.
    Hsp90-IN-48
  • HY-106031A
    F-14512 hydrochloride
    		Inhibitor
    F-14512 hydrochloride is an anticancer agent that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 hydrochloride enhances the affinity of polyamines for DNA, thereby inhibiting topoisomerase II and achieving selective cellular uptake. F-14512 hydrochloride exhibits significant cytotoxicity against cells with high PTS activity and induces DNA damage. F-14512 hydrochloride demonstrates potent antitumor activity in the MX1 breast tumor xenograft model. F-14512 hydrochloride could be used to study breast cancer.
    F-14512 hydrochloride
  • HY-175216
    Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6
    		Inhibitor
    Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6 is a drug-linker conjugate for ADC. Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6 consists of a topoisomerase 1 inhibitor (Topi MF-6) (HY-175203) and a cleavable linker (Maleimide-Ph(3,5-F)-PEG4-Val-Ala) (HY-175218). Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6 can be used for synthesis of ADCs.
    Maleimide-Ph(3,5-F)-PEG4-Val-Ala-MF-6
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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