2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Topoisomerase

Topoisomerase

Topoisomerase

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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:

Topoisomerase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-145397
    (4-NH2)-Exatecan
    		Inhibitor 99.93%
    (4-NH2)-Exatecan (compound A), a topoisomerase inhibitor, is a derivative of Exatecan. (4-NH2)-Exatecan can be used in the synthesis of antibody-drug conjugates (ADCs).
    (4-NH2)-Exatecan
  • HY-13631J
    (1R,9R)-Exatecan mesylate
    		Inhibitor 99.49%
    (1R,9R)-Exatecan mesylate ((1R,9R)-DX8951f) is a non-prodrug camptothecin derivative and a potent topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1R,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1R,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. (1R,9R)-Exatecan mesylate is widely used in preclinical studies of multiple cancers including pancreatic cancer, lung cancer, breast cancer, and leukemia. The low-activity isomer of (1R,9R)-Exatecan mesylate is (1S,9R)-Exatecan mesylate (HY-13631I).
    (1R,9R)-Exatecan mesylate
  • HY-N0498
    Nitidine chloride
    		Inhibitor 99.82%
    Nitidine 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.
    Nitidine chloride
  • HY-13725
    Pirarubicin
    		Inhibitor 99.61%
    Pirarubicin is an anthracycline antibiotics, acts as a topoisomerase II inhibitor, and is a widely used for treatment of various cancers, in particular, solid tumors.
    Pirarubicin
  • HY-118590
    ICRF-193
    		Inhibitor 99.64%
    ICRF-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.
    ICRF-193
  • HY-15753
    Ellipticine
    		Inhibitor 99.59%
    Ellipticine (NSC 71795) is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.
    Ellipticine
  • HY-145399
    AZ14170133
    		Inhibitor 99.73%
    AZ14170133 (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.
    AZ14170133
  • HY-13566A
    Belotecan hydrochloride
    		Inhibitor 99.97%
    Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic camptothecin derivative.
    Belotecan hydrochloride
  • HY-N0716A
    Berberine hemisulfate
    		Inhibitor 99.63%
    Berberine hemisulfate is the hemisulfate form of Berberine (HY-N0716). Berberine hemisulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian. Berberine hemisulfate exhibits anti-inflammatory, antibiobic, antitumor, cardiovascular protective and neuroprotective activity.
    Berberine hemisulfate
  • HY-147271
    Mal-PEG8-Val-Ala-PAB-Exatecan
    		Inhibitor 99.48%
    Mal-PEG8-Val-Ala-PAB-Exatecan (Compound 9b) is an antibody-drug conjugate linker (ADC linker) that binds to Nectin-4 polypeptides conjugated to chemotherapeutic agents. Mal-PEG8-Val-Ala-PAB-Exatecan can be used for cancer research.
    Mal-PEG8-Val-Ala-PAB-Exatecan
  • HY-17577
    Berberine chloride hydrate
    		Inhibitor 99.82%
    Berberine 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.
    Berberine chloride hydrate
  • HY-13631I
    (1S,9R)-Exatecan mesylate
    		Inhibitor 99.11%
    (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).
    (1S,9R)-Exatecan mesylate
  • HY-13631AG
    Exatecan mesylate (GMP)
    		Inhibitor
    Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
    Exatecan mesylate (GMP)
  • HY-44369
    Exatecan Intermediate 6
    		Inhibitor 98.98%
    Exatecan 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).
    Exatecan Intermediate 6
  • HY-177434
    Precemtabart tocentecan
    		Inhibitor 99.31%
    Precemtabart 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.
    Precemtabart tocentecan
  • HY-13727A
    Pixantrone
    		Inhibitor 98.75%
    Pixantrone (BBR 2778) dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
    Pixantrone
  • HY-13725A
    Pirarubicin Hydrochloride
    		Inhibitor 99.14%
    Pirarubicin 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.
    Pirarubicin Hydrochloride
  • HY-148668
    MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan
    		Inhibitor
    MC-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).
    MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan
  • HY-13562A
    Banoxantrone dihydrochloride
    		Inhibitor 99.46%
    Banoxantrone dihydrochloride is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
    Banoxantrone dihydrochloride
  • HY-N2331
    Proscillaridin A
    		Inhibitor 99.74%
    Proscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively.
    Proscillaridin A
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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