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
(769)
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Topoisomerase Agonists
(2)
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Topoisomerase Modulator
(1)
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Topoisomerase Inducer
(1)
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Topoisomerase Degraders
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Topoisomerase Controls
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Topoisomerase Ligands
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Topoisomerase Proteins
(1)
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DNA topoisomerase II Proteins
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Topoisomerase Related Products (847)
Related Products (847)
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Recombinant Proteins (1)
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Antibodies (4)
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Topoisomerase Isoform Comparison
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Merbarone
0 ImagesSynonyms: NSC 336628Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage without stabilizing topo II-DNA covalent complexes. Merbarone is an anticancer agent.
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Flumequine
0 ImagesSynonyms: R-802Flumequine (R-802) is a quinolone antibiotic, and acts as a topoisomerase II inhibitor, with an IC50 of 15 μM (3.92 μg/mL).
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Bisantrene
0 ImagesSynonyms: CL216942Bisantrene is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene targets eukaryotic type II topoisomerases. Bisantrene is a substrate of MDR1.
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Amonafide
0 ImagesSynonyms: AS1413Amonafide is a topoisomerase II inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA.
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PluriSIn #2
0 ImagesPluriSIn #2 is a selective transcriptional inhibitor of topoisomerase II α (TOP2A). PluriSIn #2 is a compound that selectively eliminates undifferentiated human pluripotent stem cells (hPSCs).
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Lomefloxacin hydrochloride
0 ImagesSynonyms: SC47111A hydrochloride; NY-198 hydrochlorideLomefloxacin hydrochloride (NY-198 hydrochloride) is an orally active difluoroquinolone antibiotic. Lomefloxacin hydrochloride prevents DNA supercoiling and replication by inhibiting bacterial topoisomerase II. Lomefloxacin hydrochloride induces ROS production and Apoptosis. Lomefloxacin hydrochloride has broad-spectrum bactericidal activity against Gram-positive and Gram-negative bacteria. Lomefloxacin hydrochloride has anticancer effects against melanoma. Lomefloxacin hydrochloride can be used in the study of systemic bacterial infections (such as Salmonella typhimurium infections), skin and melanoma .
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SN-38 (Standard)
0 ImagesSynonyms: 7-Ethyl-10-hydroxycamptothecin (Standard)SN-38 (Standard) is the analytical standard of SN-38. This product is intended for research and analytical applications. SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254).
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Gly-Gly-Phe-Gly-NH-O-CO-Exatecan hydrochloride
0 ImagesGly-Gly-Phe-Gly-NH-O-CO-Exatecan, as a drug-linker conjugate composed of linker Gly-Gly-Phe-Gly-NH-O-CO and Exatecan, can be used to prepare antibody conjugate drugs. Exatecan is a DNA topoisomerase I inhibitor that can be used in cancer research.
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Levofloxacin hydrochloride
0 ImagesSynonyms: (-)-Ofloxacin hydrochlorideLevofloxacin hydrochloride is an orally active antibiotic. Levofloxacin inhibits DNA gyrase and topoisomerase IV activity, inducing Apoptosis. Levofloxacin hydrochloride has antibacterial activity against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrochloride exhibits anticancer activity against lung cancer. Levofloxacin hydrochloride has anti-acnegenic, anxiogenic, and analgesic effects. Levofloxacin hydrochloride shortens sleep duration in mice. Levofloxacin hydrochloride can be used in the research of infectious diseases (such as tuberculosis, chronic periodontitis, bacterial infections associated with stable COPD, and BK viremia) and lung cancer.
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Levofloxacin (Standard)
0 ImagesSynonyms: (-)-Ofloxacin (Standard)Levofloxacin (Standard) is the analytical standard of Levofloxacin. This product is intended for research and analytical applications. Levofloxacin ((-)-Ofloxacin) is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin inhibits the DNA gyrase and topoisomerase IV. Levofloxacin can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin shows anti-orthopoxvirus activity.
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FZ-AD005
0 ImagesCat. No.: HY-164729FZ-AD005 is a DLL3-targeting antibody-drug conjugate (ADC) with high selectivity, composed of the anti-DLL3 antibody FZ-A038 (HY-P990896), a dipeptide linker (Val-Ala), and DXd (HY-13631D). The Kd value of FZ-AD005 for human DLL3 ranges from 13.29 to 58.3 pmol/L. After binding to DLL3 on the cell surface, FZ-AD005 mediates endocytosis, and the payload DXd is released via cleavage by lysosomal cathepsins. DXd inhibits topoisomerase TopI to induce double-strand DNA breaks, cell cycle arrest and apoptosis, and FZ-AD005 exhibits bystander killing activity against adjacent DLL3-negative cells. FZ-AD005 shows stable circulation in vivo, has good tolerance and acceptable pharmacokinetic profiles in rats and cynomolgus monkeys, and effectively inhibits the growth of DLL3-expressing tumor cells. FZ-AD005 serves as a promising candidate molecule for research on small cell lung cancer and human neuroendocrine prostate cancer.
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Ac-Exatecan
0 ImagesAc-Exatecan is acetylation-modified Exatecan (HY-13631). Exatecan is a common toxin component in ADC preparation (ADC cytotoxin) and an inhibitor of DNA topoisomerase I (IC50 = 2.2 μM). Exatecan has antitumor activity. Exatecan can be used as a payload for ADC. Exatecan is effective against P-glycoprotein mediated multi-drug resistant cells.
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MC-GGFG-PAB-Exatecan
0 ImagesMC-GGFG-PAB-Exatecan is a linker-drug conjugate, consisting of the MC-GGFG-PAB (HY-136432) linker and the Topoisomerase I inhibitor Exatecan (HY-13631). MC-GGFG-PAB-Exatecan can be used to synthesize antibody-drug conjugates (ADCs). MC-GGFG-PAB-Exatecan applies to cancer research.
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Genz-644282
0 ImagesGenz-644282 is a non-camptothecin topoisomerase I inhibitor, used for cancer research.
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Mc-PEG4-Val-Ala-PAB-Exatecan
0 ImagesCat. No.: HY-171580Purity: 99.65%Mc-PEG4-Val-Ala-PAB-Exatecan is a Drug-linker conjugate for ADC. Mc-PEG4-Val-Ala-PAB-Exatecan contains the ADC linker (Mc-PEG4-Val-Ala-PAB) and a DNA topoisomerase I inhibitor Exatecan (HY-13631).
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Topobexin
0 ImagesTopobexin is a TOP2B-selective inhibitor with IC50 values of 0.19 μM and 4.8 μM for TOP2B and TOP2A (DNA decatenation assay). Topobexin binds to non-homologous residues in the obex pocket and targets the ATPase domain of TOP2B. Topobexin prevents anthracycline-induced DNA double-strand break formation, apoptotic signaling mediated by caspase 3/7, 8 and 9, cardiomyocyte morphological changes, mitochondrial depolarization/loss, left ventricular systolic dysfunction, extracellular matrix remodeling, fibrotic alterations, and increases in plasma cardiac troponin T and BNP. Topobexin does not impair the antiproliferative effects of anthracyclines in cancer cells, exhibits no intrinsic cytotoxicity in cardiomyocytes, and is well tolerated in rabbits. Topobexin can be used in studies related to anthracycline-induced cardiotoxicity.
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(R)-Exatecan Intermediate 1
0 ImagesCat. No.: HY-42487BCAS No.: 110351-91-2(R)-Exatecan Intermediate 1 is a key intermediate in the synthesis of Camptothecin (HY-16560) derivatives, and can be used to prepare Exatecan mesylate (DX8951f) (HY-13631A). (R)-Exatecan Intermediate 1 enables the synthesis of Exatecan, which exhibits low sensitivity to multidrug resistance and has great value in anti-tumor research.
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Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan
![Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan](https://file.medchemexpress.com/product_pic/hy-173634.gif "Click to View Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan Product Detail")
0 ImagesMal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan (LP1) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB (HY-173635) to make antibody agent conjugate (ADC), AZD0516 (HY-173639).
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Coralyne chloride
0 ImagesCoralyne chloride is a protoberberine alkaloid with potent anti-cancer activities. Coralyne chloride acts as a potent topoisomerase I poison and induces Top I mediated DNA cleavage. Coralyne chloride can be used for preparing coralyne derivatives as DNA binding fluorescent probes.
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Etoposide (Standard)
0 ImagesSynonyms: VP-16 (Standard); VP-16-213 (Standard)Etoposide (Standard) is the analytical standard of Etoposide. This product is intended for research and analytical applications. Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy.
