2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Topoisomerase
  5. Topo I Isoform
  6. Topo I Inhibitor

Topo I Inhibitor

Topo I Inhibitors (90):

Cat. No. Product Name Effect Purity
  • HY-125930
    T-2513
    		Inhibitor
    T-2513 is a selective topoisomerase I inhibitor. T-2513 binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death.
  • HY-105387
    Heliquinomycin
    		Inhibitor
    Heliquinomycin is an inhibitor of DNA helicase (Ki: 6.8 μM) and inhibits DNA and RNA synthesis. Heliquinomycin is effective against Gram-positive bacteria strains. Heliquinomycin inhibits cancer cell growth.
  • HY-P10765
    DTS-108
    		Inhibitor
    DTS-108 is a prodrug of SN38 (HY-13704) (a Topoisomerase I inhibitor). DTS-108 is a conjugate generated by linking SN38 to a human oligopeptide via an esterase sensitive cross-linker. DTS-108 exhibits anti-tumor activity against colorectal, lung, and mammary cancer.
  • HY-147698
    ZLHQ-5f
    		Inhibitor
    ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile.
  • HY-161501
    3-Fluoro-evodiamine glucose
    		Inhibitor
    3-Fluoro-evodiamine glucose (Compound 8) is an evodiamine-glucose conjugate. 3-Fluoro-evodiamine glucose activates the expression of glucose transporter 1 (GLUT1), and inhibits topoisomerase I/II. 3-Fluoro-evodiamine glucose induces apoptosis and arrests the cell cycle at G2/M phase. 3-Fluoro-evodiamine glucose exhibits antitumor efficacy in vivo and in vitro, without significant toxicity.
  • HY-145859
    Topo I-IN-1
    		Inhibitor
    Topo I-IN-1 (Compound 14d) is a potent Topo I inhibitor with antitumor activity and DNA intercalative capability. Topo I-IN-1 induces cell apoptosis.
  • HY-168632
    Topoisomerase I/II inhibitor 6
    		Inhibitor
    Topoisomerase I/II inhibitor 6 (compound 3i) is a potent inhibitor of topoisomerase I and II with IC50s of 4.77 and 15 µM, respectively. Topoisomerase I/II inhibitor 6 shows antiproliferative activities against human melanoma LOX IMVI cancer cell line with IC50 values of 26.7 and 25.4 µM, respectively. Topoisomerase I/II inhibitor 6 provokes substantial levels of early, late apoptosis and increases the expression level of active caspase-3.
  • HY-145852
    Top/HDAC-IN-2
    		Inhibitor
    Top/HDAC-IN-2 (45b), a Top and HDAC dual inhibitor, exhibits potent antitumor activities and induces apoptosis.
  • HY-168739
    Topoisomerase I inhibitor 17
    		Inhibitor
    Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice.
  • HY-13622A
    Elomotecan
    		Inhibitor
    Elomotecan (BN 80927 free base) is a potent inhibitor of topoisomerases I and II. Elomotecan is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan reduces the proliferation of different tumor cells with higher potency than other anticancer agents of reference targeting topoisomerases I and II.
  • HY-168285
    LE01
    		Inhibitor
    LE01 is a drug-linker conjugate for ADC. LE01 contains a ADC linker and a DNA topoisomerase I inhibitor DXd (HY-13631D). LE01 can be used to synthesize HER2-targeting ADC (HER2-LE01).
  • HY-143265
    Topoisomerase I inhibitor 2
    		Inhibitor
    Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect.
  • HY-162805
    iNOS/TopoI-IN-1
    		Inhibitor
    iNOS/TopoI-IN-1 (compound AuL9) is a multi-target hybrid molecule with anti-tumor, anti-inflammatory and antioxidant activities. iNOS/TopoI-IN-1 inhibits the growth of breast cancer cells MCF-7 and MDA MB-231 in vitro with IC50 of 3.5 μM and 6.3 μM, respectively, and induces DNA damage and apoptosis of breast cancer cells by inhibiting human topoisomerase I (TopoI) (Ki=2.72 μM). In addition, NOS/TopoI-IN-1 inhibits the expression of iNOS by inhibiting the activation of NF-kB (Ki=1.49 μM).
  • HY-N10115
    Huanglongmycin N
    		Inhibitor
    Huanglongmycin N is a DNA topoisomerase I inhibitor (EC50 = 14 μM).
  • HY-171124
    Tilatamig samrotecan
    		Inhibitor
    Tilatamig samrotecan (AZD9592) is an antibody-drug conjugate (ADC) used to deliver topoisomerase I inhibitors (TOP1i), targeting the epidermal growth factor receptor (EGFR) and c-MET, with anti-tumor activity. Tilatamig samrotecan (AZD9592) can induce DNA double-strand breaks, increase the expression of pRAD50 and γH2AX, and inhibit the growth of non-small cell lung cancer.
  • HY-164836
    Deruxtecan-Eribulin
    		Inhibitor
    Deruxtecan-Eribulin is a Drug-Linker Conjugates for ADC, which is composed of a linker and a toxic molecule Exatecan (HY-13631) (DNA topoisomerase I inhibitor) and Eribulin (HY-13442) (Microtubule inhibitor). Deruxtecan-Eribulin can be used for ADC synthesis.
  • HY-161628
    Tapcin
    		Inhibitor
    Tapcin is a dual inhibitor for topoisomerase I and topoisomerase II, with IC50 of 203 and 71 nM. Tapcin inhibits proliferations of cancer cells A-375, HeLa, Huh7.5, U2-OS, A549, Caco-2 and HT29, with IC50s of 441, 1.04, 40.5, 0.002, 0.006, 0.287 and 0.842 nM, respectively. Tapcin exhibits antitumor activity in HT29 xenograft model.
  • HY-161082
    Topoisomerase I inhibitor 12
    		Inhibitor
    Topoisomerase I inhibitor 12 (compound 12), a Camptothecin (HY-16560)-based derivative, is a potent Topoisomerase I inhibitor. Topoisomerase I inhibitor 12 shows anticancer activity.
  • HY-143402
    Topoisomerase I/II inhibitor 2
    		Inhibitor
    Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer.
  • HY-170912
    Topo I/II-IN-2
    		Inhibitor
    Topo I/II-IN-2 (Compound 3g) is an inhibitor of Topo I and Topo II. Topo I/II-IN-2 inhibits NCI-H446 cells and NCI-H1048 cells with IC50s of 1.30 μM and 1.42 μM, respectively. Topo I/II-IN-2 induces mitochondrial Apoptosis, mitochondrial dysfunction and activity generation. Topo I/II-IN-2 inhibits the PI3K/Akt/mTOR pathway. Topo I/II-IN-2 prevents SCLC (small cell lung cancer) cell proliferation, invasion, and migration in vitro. .