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
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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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Nitidine chloride
0 ImagesNitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway, also has anti-inflammatory activity. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.
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ICRF-193
0 ImagesICRF-193 is a DNA Topoisomerase II inhibitor. (S,S)- and (R,R)-isomers ICRF-193 make up an racemic mixture, ICRF-196 (HY-118590A). ICRF-193 can inhibit DNA syntheses and induces apoptosis. ICRF-193 exhibits anti-cancer and anti-inflammation effects. ICRF-193 shows cardioprotective effect against anthracycline toxicity to cardiomyocytes. ICRF-193 can be used for the researches of cancer, infection, inflammation and cardiovascular disease, such as acute promyelocytic leukemia.
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AZ14170133
0 ImagesSynonyms: SG 3932; AZ-0133AZ14170133 (SG 3932; AZ-0133) is a Drug-Linker Conjugates for ADC. AZ14170133 consists of the ADC cytotoxic payload topoisomerase 1 inhibitor and a linker. AZ14170133 can be used for synthesis of ADC AZD9592 (HY-171124) and AZD 8205 (HY-171689). AZ14170133 can be used for the research of cancer.
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Ellipticine
0 ImagesEllipticine (NSC 71795) is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.
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(1S,9R)-Exatecan mesylate
0 ImagesSynonyms: (1S,9R)-DX8951f(1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is a non-prodrug camptothecin derivative and a topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1S,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1S,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1S,9R)-Exatecan mesylate is widely used in preclinical studies of various cancers such as pancreatic cancer, lung cancer, breast cancer, and leukemia.
The chiral isomer of (1S,9R)-Exatecan mesylate is (1R,9R)-Exatecan mesylate (HY-13631J).
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Pirarubicin
0 ImagesSynonyms: THPPirarubicin is an anthracycline antibiotics, acts as a topoisomerase II inhibitor, and is a widely used for treatment of various cancers, in particular, solid tumors.
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Precemtabart tocentecan
0 ImagesSynonyms: Precem-TcT; M 9140Precemtabart tocentecan (Precem-TcT; M 9140) is an anti-CEACAM5 (carcinoembryonic antigen-related cell adhesion molecule 5) antibody-drug conjugate (ADC). Precemtabart tocentecan consists of a tumor-specific anti-CEACAM5 monoclonal antibody Precemtabart (HY-P990940), a highly hydrophilic and stable cleavable β-glucuronide linker, and a topoisomerase 1 inhibitor payload Exatecan (HY-13631), and the drug-linker conjugate for ADC is Mal-Gly-PAB-Exatecan-D-glucuronic acid (HY-153179). Precemtabart tocentecan inhibits the growth of CEACAM5-positive cancer cells. Precemtabart tocentecan exhibits significant antitumor activity in CEACAM5-expressing xenograft models. Precemtabart tocentecan can be used for the study of CEACAM5-expressing advanced solid tumors, especially mCRC.
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Berberine chloride hydrate
0 ImagesSynonyms: Natural Yellow 18 chloride hydrateBerberine chloride hydrate (Natural Yellow 18 chloride hydrate) is an alkaloid that acts as an antibiotic. Berberine chloride hydrate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties.
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Belotecan hydrochloride
0 ImagesSynonyms: CKD-602Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic camptothecin derivative.
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Exatecan mesylate (GMP)
0 ImagesCat. No.: HY-13631AGCAS No.: 169869-90-3Synonyms: DX8951f (GMP)
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Exatecan Intermediate 6
0 ImagesExatecan Intermediate 6 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 6 can be used to synthesize Antibody-Drug Conjugates (ADCs).
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Pixantrone
0 ImagesSynonyms: BBR 2778Pixantrone (BBR 2778) dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
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MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan
0 ImagesSynonyms: SHR-A1811 Drug-linkerMC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan (SHR-A1811 Drug-linker) is a agent-linker conjugates for ADC, consisting Exatecan (HY-13631). Exatecan is a DNA Topoisomerase I inhibitor (IC50=2.2 μM).
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Idarubicin
0 ImagesSynonyms: 4-DemethoxydaunorubicinIdarubicin is an orally active and potent anthracycline antileukemic agent. Idarubicin inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription. Idarubicin shows induction of DNA damage. Idarubicin inhibits DNA synthesis and of c-myc expression. Idarubicin inhibits the growth of bacteria and yeasts.
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Pirarubicin Hydrochloride
0 ImagesSynonyms: THP HydrochloridePirarubicin Hydrochloride is an anthracycline antibiotics, acts as a topoisomerase II inhibitor, and is a widely used for treatment of various cancers, in particular, solid tumors.
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ABBV-706
0 ImagesCat. No.: HY-170554Purity: 99.71%ABBV-706 is a SEZ6-targeted topoisomerase 1 inhibitor Antibody-Drug Conjugates (ADCs), which is composed of the Linker-Payload conjugation (HY-148820) and the Anti-SEZ6 Antibody (SC17) (HY-P991041). ABBV-706 can inhibit cancer cells proliferation and induce DNA damage and G2/M arrest. ABBV-706 exhibits high efficacy against small cell lung cancer (SCLC), neuroendocrine tumors (NENs) and central nervous system (CNS) tumors.
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Topotecan
0 ImagesSynonyms: SKF 104864A; NSC 609669Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity.
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Proscillaridin A
0 ImagesProscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively.
