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
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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 (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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Gatifloxacin
0 ImagesSynonyms: AM-1155; BMS-206584; PD135432Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic that can cross the blood-brain barrier, with broad-spectrum antibacterial activity. Gatifloxacin inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50=0.109 μg/ml). Gatifloxacin can be used to treat bacterial conjunctivitis in vivo.
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NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT hydrochloride
![NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT hydrochloride](https://file.medchemexpress.com/product_pic/hy-148819a.gif "Click to View NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT hydrochloride Product Detail")
0 ImagesCat. No.: HY-148819APurity: 98.46%NH2-bicyclopentane-7-MAD-MDCPT hydrochloride (Formula I) is a topoisomerase I (TOP1) inhibitor. NH2-bicyclopentane-7-MAD-MDCPT hydrochloride is applicable to the synthesis of the ADC ABBV-969. NH2-bicyclopentane-7-MAD-MDCPT hydrochloride is used in research on lung adenocarcinoma and melanoma.
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Banoxantrone dihydrochloride
0 ImagesSynonyms: AQ4N dihydrochlorideBanoxantrone dihydrochloride is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
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Belotecan
0 ImagesSynonyms: CKD-602 free baseBelotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer.
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DBCO-PEG3-VC-Exatecan
0 ImagesDBCO-PEG3-VC-Exatecan (compound 25) is a Drug-Linker Conjugate for ADC. DBCO-PEG3-VC-Exatecan contains the ADC linker (DBCO-PEG3-VC) and a DNA topoisomerase I inhibitor Exatecan (HY-13631).
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Precemtabart
0 ImagesSynonyms: MBE-748; M-9140 Antibody; MBE-2882 AntibodyPrecemtabart is a humanized IgG1 antibody targeting CEACAM5, with selectivity for CEACAM5-positive cells. Precemtabart binds to CEACAM5 on tumor cells to deliver the topoisomerase 1 inhibitor Exatecan (HY-13631), and induces cell death by inhibiting the function of TOP1. Precemtabart inhibits the growth of CEACAM5-positive cancer cells. Precemtabart causes dose-dependent hematolymphoid and intestinal-related effects in cynomolgus monkeys. Precemtabart can be used in research related to metastatic colorectal cancer, metastatic pancreatic ductal carcinoma, advanced gastric cancer, advanced non-small cell lung cancer, and advanced pancreatic adenocarcinoma.
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(S)-10-Hydroxycamptothecin
0 ImagesSynonyms: 10-HCPT; 10-Hydroxycamptothecin(S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment.
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DS-3939a
0 ImagesCat. No.: HY-177442Purity: 99.15%Synonyms: DS-3939DS-3939a (DS-3939) is an anti-TA-MUC1 (tumor-associated mucin-1) antibody-drug conjugate (ADC). DS-3939a consists of a humanized anti-TA-MUC1 IgG1 monoclonal antibody Gatipotuzumab ( HY-P99634), a stable and cleavable tetrapeptide-based linker (Gly-Gly-Phe-Gly), and a DNA topoisomerase I inhibitor payload (DXd) (HY-13631D), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). DS-3939a inhibits the growth of TA-MUC1-positive cancer cells (CFPAC-1, NCI-H2110) by inducing DNA damage and apoptosis. DS-3939a exhibits significant antitumor activity in a variety of TA-MUC1-expressing advanced solid tumors. DS-3939a can be used for the study of TA-MUC1-expressing advanced cancers.
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NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
![NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT](https://file.medchemexpress.com/product_pic/hy-148819.gif "Click to View NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT Product Detail")
0 ImagesNH2-bicyclopentane-7-MAD-MDCPT (Formula I) is a topoisomerase I (TOP1) inhibitor. NH2-bicyclopentane-7-MAD-MDCPT is applicable to the synthesis of the ADC ABBV-969. NH2-bicyclopentane-7-MAD-MDCPT is used in research on lung adenocarcinoma and melanoma.
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Cholesterol hemisuccinate Tris salt
0 ImagesSynonyms: Cholesterol hydrogen succinate Tris salt; CHS-TrisCholesterol hemisuccinate (Cholesterol hydrogen succinate) Tris salt is a compound with hepatoprotective and anticancer activity. Cholesterol hemisuccinate Tris salt inhibits Acetaminophen (AAP) (HY-66005) hepatotoxicity, and prevents AAP-induced hepatic apoptosis and necrosis. Cholesterol hemisuccinate Tris salt inhibits DNA polymerase and DNA topoisomerase to inhibit DNA replication and repair and cell division. Cholesterol hemisuccinate Tris salt inhibits tumor growth. Cholesterol hemisuccinate Tris salt can be used for buffer preparation.
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Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan
0 ImagesMal-PEG2-Gly-Gly-Phe-Gly-Exatecan is a bioactive drug-linker conjugate for ADC (Drug-Linker Conjugates for ADC). Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan consists of Exatecan (HY-13631) and a linker. Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan is applicable to ADC synthesis and cancer research. Exatecan acts as a DNA Topoisomerase I inhibitor.
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SN-38-d3
0 ImagesSynonyms: NK012-d3SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively.
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Val-Ala-PABC-Exatecan
0 ImagesVal-Ala-PABC-Exatecan is a Drug-Linker Conjugates for ADC, consiting of a cleavable Tesirine linker (Val-Ala-PABC) and Exatecan (HY-13631) (topoisomerase I inhibitor). Val-Ala-PABC-Exatecan can be used for ADC molecues synthesis, such as Mal-PEGn-amide-va-Exatecan.
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Tilatamig samrotecan
0 ImagesCat. No.: HY-171124Synonyms: AZD9592Tilatamig samrotecan (AZD9592) is an anti-EGFR/c-MET antibody-drug conjugate (ADC). Tilatamig samrotecan consists of an anti-EGFR/c-MET antibody with the drug-linker conjugate being AZ14170133 (HY-145399) (a topoisomerase I (TOP1i) inhibitor payload). Tilatamig samrotecan induces multiple DNA damage response pathway markers (like ATM, ATR, γH2AX). Tilatamig samrotecan selectively binds to EGFR and c-MET, delivering the cytotoxic payload. Tilatamig samrotecan exerts anti-tumor activity in vivo. Tilatamig samrotecan can be used for non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) research.
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MC-GGFG-AM-(10Me-11F-Camptothecin)
0 ImagesMC-GGFG-AM-(10Me-11F-Camptothecin) is a linker-payload conjugate used to synthesize ZW251. ZW251 an antibody-drug conjugate (ADC) targeting human GPC3. ZW251 consists of a humanized IgG1 antibody conjugated to a novel camptothecin-based topoisomerase 1 inhibitor, ZD06519, via a linker. The linker is the maleimide anchor and a glycyl glycyl phenylalanyl glycine (GGFG)-aminomethyl (AM) cleavable linker. ZW251 has high affinity with human and cynomolgus monkey GPC3. ZW251 displays rapid internalization in GPC3-expressing HCC cell lines, and bystander-mediated killing of GPC3 negative cancer cells.
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Puxitatug samrotecan
0 ImagesSynonyms: AZD 8205; P-SamPuxitatug samrotecan (AZD 8205) is an antibody-drug conjugate (ADC) targeting B7-H4, formed by the random conjugation of the Puxitatug (HY-P990059) antibody and AZ14170133 (HY-145399) via interchain cysteine reduction. Puxitatug samrotecan binds to B7-H4 to deliver the payload to B7-H4-expressing cells, inhibits topoisomerase I, and induces cytotoxicity in cancer cells and xenograft models. Puxitatug samrotecan can be used in studies of B7-H4-expressing tumors.
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Amsacrine
0 ImagesSynonyms: m-AMSA; acridinyl anisidideAmsacrine (m-AMSA; acridinyl anisidide) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
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Artemisitene
0 ImagesArtemisitene, a natural derivative of Artemisinin, is a Nrf2 activator with antioxidant and anticancer activities. Artemisitene activates Nrf2 by decreasing Nrf2 ubiquitination and increasing its stability.
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(αR)-Cyclopropaneacetamide-Exatecan
0 ImagesSynonyms: SHR169265(αR)-Cyclopropaneacetamide-Exatecan (SHR169265) is a DNA Topoisomerase I inhibitor with enhanced membrane permeability (with an IC50 of 1.34 μM against the human DNA Topoisomerase I). (αR)-Cyclopropaneacetamide-Exatecan exerts cytotoxic effects by inhibiting the enzymatic activity of Topoisomerase I, and this anticancer effect is independent of the expression level of HER2. (αR)-Cyclopropaneacetamide-Exatecan is an ADC Cytotoxin derived from Exatecan (HY-13631), which can be used in research related to advanced cancers such as breast cancer, gastric cancer, colorectal cancer and non-small cell lung cancer.
