2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Topoisomerase
  5. Topo II Isoform

Topo II

Topoisomerase II (Topo II) is a nuclear enzyme that modulates DNA topology by inducing transient double-strand breaks and facilitating chromosomal segregation during mitosis[1][2]. Mechanistically, Topo IIα primarily associates with proliferating cells, regulating cell division, whereas Topo IIβ participates in differentiation and transcriptional regulation[2][3]. In disease contexts, aberrant Topo II activity or inhibition can induce DNA double-strand breaks, contributing to infant leukemia through MLL gene rearrangements during fetal development[4][5]. Clinical evidence indicates that inhibitors of Topo II, such as anthracyclines, selectively target Topo IIα to exert cytotoxic effects in hematological malignancies, but off-target inhibition of Topo IIβ mediates cardiotoxicity[6][7]. Compared with Topo IIα, Topo IIβ displays distinct expression patterns and immunophenotype associations in acute myeloid leukemia, reflecting unique biological roles[3]. Isoform-specific inhibitors, such as topobexin, exploit structural differences in the ATPase domains of Topo IIα and Topo IIβ, enabling selective inhibition of Topo IIβ and protection against anthracycline-induced cardiac damage[7]. Mechanistic studies further reveal that cellular resistance to Topo II inhibitors involves post-translational modifications, including phosphorylation, and signaling pathways that modulate DNA damage responses[2]. Collectively, these findings highlight Topo II isoforms as critical molecular targets with distinct functional roles, disease relevance, and therapeutic implications for selective drug design[2][7].

Cat. No. Product Name Effect Purity
  • HY-15142
    Doxorubicin hydrochloride
    		Inhibitor 99.90%
    Doxorubicin hydrochloride (Hydroxydaunorubicin hydrochloride; ADR), 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.
  • HY-13629
    Etoposide
    		Inhibitor 99.93%
    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.
  • HY-13502
    Mitoxantrone
    		Inhibitor 99.58%
    Mitoxantrone is a potent topoisomerase II inhibitor. Mitoxantrone also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone shows antitumor activity. Mitoxantrone also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.
  • HY-13062
    Daunorubicin hydrochloride
    		Inhibitor 99.67%
    Daunorubicin (Daunomycin) hydrochloride is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin hydrochloride inhibits DNA and RNA synthesis. Daunorubicin hydrochloride is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin hydrochloride is also an anthracycline antibiotic. Daunorubicin hydrochloride can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
  • HY-17381
    Idarubicin hydrochloride
    		Inhibitor 99.94%
    Idarubicin 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.
  • HY-N17442
    Echinoside A
    		Inhibitor
    Echinoside A is a saponin. Echinoside A can be isolated from sea cucumber. Echinoside A inhibits the catalytic activity of Top2α, reduces the noncovalent binding of Top2α to DNA. Echinoside A activates Caspase-3 and induces PARP cleavage. Echinoside A induces Apoptosis. Echinoside A has anticancer activity against prostate cancer, hepatocellular carcinoma, and S-180 sarcoma. Echinoside A exhibits antifungal activity against a variety of fungi, with a minimum growth inhibitory concentration range of 3.12 to 50.0 μg/mL, including potent activity against Aspergillus and Penicillium species.
  • HY-120679A
    XK469 sodium
    		Inhibitor
    XK469 (NSC 697887) sodium is a quinoxaline-based topoisomerase II inhibitor. XK469 sodium exhibits antiproliferative activity against neuroblastoma cells. XK469 sodium can be used in the research of neuroblastoma.
  • HY-182926
    Topoisomerase I/II-IN-9
    		Inhibitor
    Topoisomerase I/II-IN-9 is a topoisomerase I/II inhibitor (IC50<10 μM) and a DNA damage inducer. Topoisomerase I/II-IN-9 blocks the interaction between the enzyme and DNA by binding to the DNA-binding pocket of the enzyme. Topoisomerase I/II-IN-9 activates the cGAS-STING pathway and promotes the accumulation of cytoplasmic double-stranded DNA. This further drives the production of type I interferons, CCL5, CXCL10 and interferon-stimulated genes, and induces anti-tumor immune responses in vivo. Topoisomerase I/II-IN-9 can be applied to the research of related diseases such as triple-negative breast cancer, colorectal cancer and gastric cancer.
  • HY-13630
    Etoposide phosphate
    		Inhibitor 99.44%
    Etoposide 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.
  • HY-13502A
    Mitoxantrone dihydrochloride
    		Inhibitor 98.98%
    Mitoxantrone 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.
  • HY-13761
    Teniposide
    		Inhibitor 99.00%
    Teniposide is a podophyllotoxin derivative, acts as a topoisomerase II inhibitor, and used as a chemotherapeutic agent.
  • HY-13062A
    Daunorubicin
    		Inhibitor 99.94%
    Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
  • HY-122575
    Aurintricarboxylic acid
    		Inhibitor
    Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway. Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM. Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM.
  • HY-N2306
    Aclacinomycin A
    		Inhibitor 99.30%
    Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis.
  • 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-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.
  • HY-15753
    Ellipticine
    		Inhibitor 99.59%
    Ellipticine (NSC 71795) is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.
  • HY-13727A
    Pixantrone
    		Inhibitor 98.75%
    Pixantrone (BBR 2778) dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
  • 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.
  • HY-13562A
    Banoxantrone dihydrochloride
    		Inhibitor 99.43%
    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.
Cat. No. Product Name / Synonyms Species Source