1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. G-quadruplex

G-quadruplex

G-Quadruplex nucleic acids or G-quadruplexes (G4s) are four-stranded DNA or RNA secondary structures that are formed in guanine-rich sequences. They are widely distributed in functional regions of the human genome, such as telomeres, ribosomal DNA (rDNA), transcription start sites, promoter regions and untranslated regions of mRNA, suggesting that G-quadruplex structures may play a pivotal role in the control of a variety of cellular processes. In addition, G4s are enriched and conserved in the regulatory regions of microbes, including bacteria, fungi, and viruses.

The irregular formation of G4s on some genes might cause neurodegenerative diseases and cancers. Therefore, G4s in the genome are the therapeutic targets of these diseases. Small molecules, from naturally occurring to synthetic, are exploited to specifically target G-quadruplexes and have proven to be a new class of anticancer agents.

G-quadruplex Related Products (35):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-146812
    DIZ-3
    DIZ-3 is a selective multimeric G4 ligand based on a G4-ligand-dimerizing strategy. DIZ-3 intercalates into the G4-G4 interface, stabilizing the higher-order structure. DIZ-3 induces cell cycle arrest and apoptosis, and thus inhibits cell proliferation in alternative lengthening of telomere (ALT) cancer cells.
    DIZ-3
  • HY-15794G
    Nemorubicin (GMP)
    Nemorubicin (Methoxymorpholinyl doxorubicin) GMP is a GMP-class Nemorubicin (HY-15794). Nemorubicin is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity.
    Nemorubicin (GMP)
  • HY-162852
    OAF89
    Chemical
    OAF89 is a small molecule that interacts with G-Quadruplexes (G4s) and dsDNA with an IC50 of 1.07 μM in normal lung epithelial cells BEAS-2B.
    OAF89
  • HY-152538
    Antitumor agent-85
    Antitumor agent-85 is a G-quadruplex (G4)-ligand with the ability to stabilize different G4-DNA structures. Antitumor agent-85 has highly effective anti-tumor properties.
    Antitumor agent-85
  • HY-151263
    G4/HDAC-IN-1
    Inducer
    G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer.
    G4/HDAC-IN-1
  • HY-152537
    Antitumor agent-84
    Antitumor agent-84 (compound 21a) is a G-quadruplex (G4)-ligand with the ability to stabilize different G4-DNA structures. Antitumor agent-84 has highly effective anti-tumor properties.
    Antitumor agent-84
  • HY-D2380
    H2S probe 1
    H2S probe 1 (compound 1NND) is a derivative of nitrobenzoxadiazole (NBD) with antitumor activity. H2S probe 1 is cytotoxic to human pancreatic cancer cell MIA PaCa-2 (IC50=77.9 nM) and has a high affinity for human telomeric G-quadruplex (G4) (Kd=1.72 μM). H2S probe 1 can be used in cancer research.
    H2S probe 1
  • HY-162688
    Anticancer agent 239
    Anticancer agent 239 (Compound 5) is a ligand of hTERT promoter G-quadruplex DNA structures (hTERT G4) (Kd = 1.1 μM), and downregulates hTERT expression. Anticancer agent 239 decreases telomerase activity, shortens telomere length, and induces DNA damage, acute cellular senescence, and apoptosis. Anticancer agent 239 causes mitochondrial dysfunction, disrupts iron metabolism and activates ferroptosis in cancer cells. Anticancer agent 239 inhibits tumor growth in MDA-MB-231 xenograft mouse model.
    Anticancer agent 239
  • HY-W543137
    PT-ttpy
    Pt-ttpy, a metallo-organic complex and potent G-quadruplex ligand, effectively triggers substantial telomere-related DNA damage in cancer cells by inhibiting telomerase and/or telomere functions, while also causing various chromatin abnormalities during mitosis, such as chromatin bridges, ultrafine bridges (UFBs), and double-stranded breaks (DSBs).
    PT-ttpy
  • HY-164528
    SJ26
    SJ26 is a Wnt1 inhibitor with anticancer activity. SJ26 inhibits the expression of Wnt1 and Wnt1-mediated downstream signaling pathways in a G-quadruplex structure-dependent manner to suppress the migration activity of cancer cells.
    SJ26
  • HY-112680
    Carboxypyridostatin
    Carboxypyridostatin is a G-quadruplex ligand that has a highly molecular specificity to RNA on DNA G4s, and can reduce the proliferation of adult neural stem cells and progenitor cells derived from the subventricular zone of adult mice in vitro and in vivo.
    Carboxypyridostatin
  • HY-15794A
    Nemorubicin hydrochloride
    Nemorubicin hydrochloride is a derivative of doxorubicin, and has antitumor activity. Nemorubicin hydrochloride, not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure.
    Nemorubicin hydrochloride
  • HY-161693
    Telomeric G4s ligand 1
    Telomeric G4s ligand 1 is a telomeric G-quadruplex ligand that stabilizes telomeric G4 and induces R-loop formation, leading to DNA damage responses. Telomeric G4s ligand 1 induces apoptosis and evokes immunogenic cell death (ICD) in tumor cells.
    Telomeric G4s ligand 1
  • HY-15595
    360A
    Activator
    360A is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.
    360A
  • HY-120102
    Emicoron
    Emicoron is a new promising G4 ligand and bind G-rich oncogene promoters. Emicoron possesses a marked antitumoral activity? alone or in combination with chemotherapeutics in vivo. Emicoron can be used for cancer research.
    Emicoron