Topoisomerase
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
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Topoisomerase Inhibitors
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Topoisomerase Agonists
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Topoisomerase Modulator
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Topoisomerase Inducer
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Topoisomerase Degraders
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Topoisomerase Controls
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Topoisomerase Ligands
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Topoisomerase Proteins
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DNA topoisomerase II Proteins
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Topoisomerase Related Products (838)
Related Products (838)
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Recombinant Proteins (1)
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Antibodies (4)
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Topoisomerase Isoform Comparison
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RPR121056
0 ImagesSynonyms: APCRPR121056 (APC) is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE.
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Pefloxacin
0 ImagesSynonyms: PefloxaciniumPefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies.
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Podocarpusflavone A
0 ImagesPodocarpusflavone A is a biflavonoid present in the leaves of Podocarpus henkelii, with anti-tumor, topoisomerase I inhibitory, antibacterial and antifungal activities. Podocarpusflavone A exhibits antibacterial activity against Enterococcus faecalis and Pseudomonas aeruginosa. Podocarpusflavone A shows weak activity against fungal pathogens. Podocarpusflavone A targets topoisomerase I and induces cell cycle arrest and apoptosis in MCF-7 cells. Podocarpusflavone A can be used for studies on cancer, bacterial and fungal infections.
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(±)-10-Hydroxycamptothecin
0 ImagesSynonyms: (±)-10-HCPT(±)-10-Hydroxycamptothecin is an indole alkaloid that inhibits the activity of topoisomerase I and has a broad spectrum of anticancer activity.
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Rezetecan
0 ImagesCat. No.: HY-147408Purity: 98.90%Synonyms: SHR9265Rezetecan is a topoisomerase I inhibitor with cytotoxicity. Rezetecan can serve as an antibody-drug conjugate payload (ADC Payloads), for example, it participates in the synthesis of Tizetatug rezetecan (HY-177711). Rezetecan is applicable to research related to various cancers such as breast cancer and gastric cancer.
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Eleutherin
0 ImagesEleutherin is a type of naphthoquinone derivative with the protective effect against the injury ofhuman umbilical vein endothelial cells (HUVECs), which can be isolated from the edible bulbs of Eleutherine americana (Hong-Cong).
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Topi MF-6
0 ImagesTopi MF-6 is a DNA topoisomerase I (Top1) inhibitor. Topi MF-6 can be used as an ADC payload.
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Chrysosplenetin
0 ImagesChrysosplenetin is an orally active polymethoxyflavone. Chrysosplenetin exerts anticancer effects by inhibiting topoisomerase, protecting DNA and inducing apoptosis. Chrysosplenetin acts as an antimalarial sensitizer, reverses Artemisinin (HY-B0094) resistance by inhibiting and downregulating P-glycoprotein, and enhances the efficacy of Artemisinin. Chrysosplenetin promotes bone formation by activating the Wnt/β-catenin pathway and exerts anti-osteoporotic effects.
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(rac)-Exatecan Intermediate 1
0 Images(rac)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631), a camptothecin-based anticancer agent. Exatecan inhibits tumor growth by interfering with the proliferation and division of tumor cells by interacting with DNA. Exatecan is primarily used in research into a variety of cancers including ovarian, lung and breast cancer.
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Mocertatug rezetecan (DAR6)
0 ImagesCat. No.: HY-185280CAS No.: 3042848-25-6Synonyms: HS-20089 (DAR6); GSK5733584 (DAR6)Mocertatug rezetecan (DAR6) (HS-20089 (DAR6); GSK5733584 (DAR6)) is an antibody-drug conjugate (ADC) targeting B7-H4, composed of Mocertatug (HY-P991703) and MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan (HY-148668). Mocertatug rezetecan (DAR6) delivers a TOPO1 inhibitor payload. It binds to B7-H4-expressing tumor cells, triggers ADC internalization, and induces S-phase cell cycle arrest, cytotoxicity, and bystander killing effect. Mocertatug rezetecan (DAR6) exhibits dose-dependent tumor growth inhibition in breast cancer and endometrial cancer CDX models. It can be used in research related to platinum-resistant ovarian cancer, breast cancer, endometrial cancer, cholangiocarcinoma, and cervical cancer.
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Glycyl-Exatecan-d5 hydrochloride
0 ImagesCat. No.: HY-128995ASPurity: 98.97%Synonyms: Glycyl-DX-8951-d5 hydrochloride; Exatecan analog 2-d5 hydrochlorideGlycyl-Exatecan-d5 (Glycyl-DX-8951-d5) hydrochloride is deuterium labeled Glycyl-Exatecan (HY-128995A). Glycyl-Exatecan (Glycyl-DX-8951), a derivative of Exatecan (HY-13631), is an anticancer agent. Glycyl-Exatecan has significantly antitumor activity. Glycyl-Exatecan can be used for cancers like solid tumors research.
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Namitecan
0 ImagesSynonyms: ST-1968Namitecan is a potent topoisomerase I inhibitor, with antitumor property.
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Mal-PEG8-Phe-Lys-PAB-Exatecan TFA
0 ImagesCat. No.: HY-148380APurity: 98.66%
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Mauritianin
0 ImagesMauritianin is an orally active kaempferol glycoside. Mauritianin can be isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor. Mauritianin has hepatoprotective, neuroprotective, and renoprotective activities. Mauritianin increases vascular tone when used in combination with Alcesefoliside (HY-N5049).
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Alloc-DOX
0 ImagesSynonyms: N-Alloc doxorubicinAlloc-DOX (N-Alloc doxorubicin) is a Doxorubicin (HY-15142A) prodrug. The combination of a catalyst (such as nano-palladium) and alloc-DOX leads to a decrease in cell viability and tumour growth.
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BNS-22
0 ImagesBNS-22 is a DNA topoisomerase II (TOP2) catalytic inhibitor with the IC50 values of 2.8 μM and 0.42 μM for human TOP2α and TOP2β, respectively. BNS-22 induces abnormal division and has anti-proliferative activity.
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Seconeolitsine
0 ImagesSeconeolitsine, an antibiotic, and is an inhibitor of targeting topoisomerase I (TopA). Seconeolitsine also is a new antimicrobial agent that can inhibit S. pneumoniae growth. Seconeolitsine can inhibit TopA relaxation activity with an IC50 value of 17 μM. Seconeolitsine can be used for the research of S. pneumoniae infections resistant to other antibiotics.
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meso-Tetra(4-pyridyl)porphine
0 Imagesmeso-Tetra(4-pyridyl)porphine (Compound 10) is a porphyrin derivative. meso-Tetra(4-pyridyl)porphine is a weak inhibitor of human topoisomerase I (Top1) with an EC50 value greater than 50 µM. meso-Tetra(4-pyridyl)porphine can be used in tumor research.
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Exatecan intermediate 9
0 ImagesCat. No.: HY-43565CAS No.: 2290562-59-1Exatecan intermediate 9 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM).
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Doxorubicin liposome
0 ImagesCat. No.: HY-185370Synonyms: Pegylated liposomal doxorubicin; Liposomal doxorubicin; Doxorubicin hydrochloride liposomeDoxorubicin liposome is a liposome-encapsulated form of doxorubicin hydrochloride (HY-15142). Doxorubicin hydrochloride, a cytotoxic anthracycline antibiotic, is a potent human DNA topoisomerase I and topoisomerase II inhibitor. Compared to traditional doxorubicin, liposome encapsulation reduces its cardiotoxicity and prolongs its circulation time, thus enabling it to effectively target tumor tissue.
