2. Cell Cycle/DNA Damage
  3. Topoisomerase

Topoisomerase

Topoisomerase

Related Products

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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 Related Products (359):

Cat. No. Product Name Effect Purity
  • HY-15142
    Doxorubicin hydrochloride Inhibitor
    Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy[1][2][3].
  • HY-13631D
    Dxd Inhibitor
    Dxd (Exatecan derivative for ADC) 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).
  • HY-13631A
    Exatecan mesylate Inhibitor
    Exatecan mesylate (DX8951f) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL). Exatecan mesylate can be used in cancer research.
  • HY-13629
    Etoposide Inhibitor
    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[1].
  • HY-13704
    SN-38 Inhibitor
    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[1][2][3][4].
  • HY-W010800A
    Cholesterol hemisuccinate Tris salt Inhibitor
    Cholesterol hemisuccinate Tris salt (CHS-Tris) is an ionizable anionic detergent that stabilizes large unilamellar vesicles. CHS-Tris and Lauryl Maltose Neopentyl Glycol (LMNG) or n-Dodecyl-β-D-Maltoside (DDM) are used together for the solubilization of membrane proteins while maintaining structural integrity and activity. Cholesteryl succinate also reportedly exhibits antiproliferative activity.
  • HY-N12747
    Dichlorogelignate Inhibitor
    Dichlorogelignate (compound 4) is a selective inhibitor of topoisomerase II (Topo II). Dichlorogelignate has 100% inhibition at 50 μM[1].
  • HY-158138
    TOPOI/PARP-1-IN-1 Inhibitor
    TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice was 75.4%[1].
  • HY-147271
    Mal-PEG8-Val-Ala-PAB-Exatecan Inhibitor 98.75%
    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[1].
  • HY-148668A
    MC-Gly-Gly-Phe-Gly-(S)-Cyclopropane-Exatecan Inhibitor
    MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan is a agent-linker conjugates for ADC, consisting Exatecan (HY-13631). Exatecan is a DNA Topoisomerase I inhibitor (IC50=2.2 μM)[1].
  • HY-13721
    Phenoxodiol Inhibitor
    Phenoxodiol (Idronoxil), a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner[1][2].
  • HY-13555
    β-Lapachone Inhibitor 99.99%
    β-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.
  • HY-153795
    Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan Inhibitor 99.09%
    Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan is a drug-linker conjugate for ADC. Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan consists of Exatecan (HY-13631) and a linker. Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan can be used for synthesis of ADCs and for cancer research[1].
  • 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.
  • HY-W021377
    Exatecan Intermediate 2 Inhibitor
    Exatecan Intermediate 2 (compound B) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers[1][2].
  • HY-144769
    SDOX Inhibitor
    SDOX is the Doxorubicin (DOX) proagent. The loaded DOX proagents (SDOX) which can release the parent agents DOX triggered by excessive GSH in tumor cells, minimize the unexpected side effects on normal tissues without compromising the potency[1].
  • HY-49861
    Exatecan intermediate 11 Inhibitor
    Exatecan intermediate 11 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM)[1].
  • HY-13761
    Teniposide Inhibitor 98.88%
    Teniposide is a podophyllotoxin derivative, acts as a topoisomerase II inhibitor, and used as a chemotherapeutic agent.
  • HY-13566
    Belotecan Inhibitor
    Belotecan (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[1].
  • HY-79490
    Ac-Exatecan Inhibitor 98.70%
    Ac-Exatecan is acetylated Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM)[1].