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
(761)
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Topoisomerase Agonists
(2)
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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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Ifinatamab deruxtecan
0 ImagesSynonyms: DS-7300a; MABX-9001a; I-DXdIfinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
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Epirubicin hydrochloride
0 ImagesSynonyms: 4'-Epidoxorubicin hydrochlorideEpirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
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Betulinic acid
0 ImagesBetulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties. Betulinic acid can cross the blood-brain barrier.
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Idarubicin hydrochloride
0 ImagesSynonyms: 4-Demethoxydaunorubicin hydrochlorideIdarubicin hydrochloride is an anthracycline antileukemic agent. It inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription. Idarubicin hydrochloride inhibits the growth of bacteria and yeasts.
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Mal-Gly-PAB-Exatecan-D-glucuronic acid
0 ImagesMal-Gly-PAB-Exatecan-D-glucuronic acid can be used for Antibody-Drug Conjugates (ADCs) synthesis. Mal-Gly-PAB-Exatecan-D-glucuronic acid can be used for research of tumor research and diagnosis.
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Cu(II)-Elesclomol
0 ImagesCu(II)-Elesclomol is a complex formed by Elesclomol (HY-12040) and Cu2+ (copper ions). Cu(II)-Elesclomol is also a weak inhibitor of DNA topoisomerase I. Cu(II)-Elesclomol exerts anticancer effects by inducing oxidative stress and DNA damage through copper chelation. Cu(II)-Elesclomol can inhibit tumor cell proliferation and induce cell cycle arrest and apoptosis. Cu(II)-Elesclomol can be used in the study of cancer.
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Berberine sulfate
0 ImagesBerberine sulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine sulfate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine sulfate has antineoplastic properties. The sulfate form improves bioavailability.
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Exatecan Intermediate 1
0 ImagesExatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor with anticancer effects.
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MC-GGFG-Exatecan
0 ImagesCat. No.: HY-114233CAS No.: 1600418-29-8Synonyms: MC-GGFG-DX8951MC-GGFG-Exatecan (MC-GGFG-DX8951) is a agent-linker conjugate for ADC. MC-GGFG-Exatecan is a DX8951 (a DNA topoisomerase I inhibitor) derivative with protease cleavable MC-GGFG linker. MC-GGFG-Exatecan shows antitumor activity and can be used to prepare DX8951 antibody conjugate (ADC).
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β-Lapachone
0 Imagesβ-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.
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DXd-d5
0 ImagesCat. No.: HY-13631DSPurity: 99.57%Synonyms: Exatecan-d5 derivative for ADCDXd-d5 is a deuterium labeled DXd. DXd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) .
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Etoposide phosphate
0 ImagesSynonyms: BMY-40481Etoposide phosphate (BMY-40481) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate is the phosphate ester proagent of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate induces cell cycle arrest, apoptosis, and autophagy.
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Exatecan (Standard)
0 ImagesSynonyms: DX-8951 (Standard)Exatecan (Standard) is the analytical standard of Exatecan. This product is intended for research and analytical applications. Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
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Ciprofloxacin monohydrochloride
0 ImagesSynonyms: Bay-09867 monohydrochlorideCiprofloxacin (Bay-09867) monohydrochloride is an orally active, blood-brain barrier permeable fluoroquinolone antibacterial agent. Ciprofloxacin monohydrochloride exerts bactericidal effects primarily by inhibiting topoisomerase II and IV. Ciprofloxacin monohydrochloride inhibits the proliferation of human dental pulp stem cells and chondrocytes from young rats, and also activates the Akt signaling pathway and upregulates markers such as β-catenin and Nanog to maintain the morphological characteristics of stem cells. Ciprofloxacin monohydrochloride induces significant neurotoxicity and tissue damage, including reducing serotonin and glutathione levels in the brain, inducing oxidative stress and depression-like behaviors, and causing articular cartilage damage. Ciprofloxacin monohydrochloride can be applied to research related to infections of necrotic young permanent teeth and neurotoxicity.
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Mitoxantrone dihydrochloride
0 ImagesSynonyms: Mitozantrone dihydrochloride; NSC 301739 dihydrochlorideMitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity. Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.
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BL-B01D1
0 ImagesCat. No.: HY-164702Synonyms: Izalontamab BrengitecanBL-B01D1 (Izalontamab Brengitecan) is a bispecific antibody-drug conjugate (ADC) targeting EGFR and HER3, formed by conjugating the EGFR/HER3 bispecific antibody Izalontamab (HY-P99676) to a novel TOP-I inhibitor payload Deruxtecan 2-hydroxypropanamide (HY-153891) via a cleavable linker (Mc-Gly-Gly-Phe-Gly). BL-B01D1 binds to EGFR and HER3 on the surface of tumor cells, mediates endocytosis and releases the payload, inhibits topoisomerase I, blocks DNA replication and RNA synthesis, and disrupts DNA structure. BL-B01D1 induces cell cycle S-phase arrest, apoptosis, antibody-dependent cell-mediated cytotoxicity, and tumor cell death. BL-B01D1 can be used for cancer research.
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EIDD-1931
0 ImagesEIDD-1931 (Beta-d-N4-hydroxycytidine; NHC) is a novel nucleoside analog and behaves as a potent anti-virus agent. EIDD-1931 effectively inhibits the replication activity of venezuelan equine encephalitis virus (VEEV), Chikungunya virus (CHIKV) and hepatitis C virus (HCV).
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Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
![Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT](https://file.medchemexpress.com/product_pic/hy-148820.gif "Click to View Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT Product Detail")
0 ImagesBr-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT (Formula V) is a agent-linker conjugate that composed of a potent topoisomerase I inhibitor and a linker to make an antibody agent conjugate (ADC), ABBV-969.
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Telisotuzumab Adizutecan
0 ImagesCat. No.: HY-171945CAS No.: 2850366-99-1Synonyms: ABBV-400; Temab-ATelisotuzumab Adizutecan (ABBV-400) is an anti-c-Met antibody-drug conjugate (ADC). Telisotuzumab Adizutecan is composed of the humanized anti-c-Met antibody Telisotuzumab (HY-P99391) and the topoisomerase 1 inhibitor (7-MAD-MDCPT) (HY-132162). Telisotuzumab Adizutecan exhibits significant anti-tumor activity against advanced solid tumors such as colorectal cancer, gastric cancer, and non-small cell lung cancer.
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MC-Val-Cit-PAB-Exatecan
0 ImagesSynonyms: MC-Val-Cit-PAB-DX8951MC-Val-Cit-PAB-Exatecan (MC-Val-Cit-PAB-DX8951) is a agent-linker conjugate for ADC. MC-Val-Cit-PAB-Exatecan is composed of a DNA topoisomerase I DX-8951 (HY-13631) and a cathepsin cleavable ADC linker.
