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 (15):

Cat. No. Product Name Effect Purity
  • HY-15176A
    Pyridostatin hydrochloride
    Activator 98.77%
    Pyridostatin (RR82) hydrochloride is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin hydrochloride promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin hydrochloride targets the proto-oncogene Src. Pyridostatin hydrochloride reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells.
  • HY-108477
    TMPyP4 tosylate
    Inhibitor ≥98.0%
    TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand, which inhibits the interaction between G-quadruplexes and IGF-1. TMPyP4 tosylate (TMP 1363) is a telomerase inhibitor with antitumor effects in osteosarcoma cell lines.
  • HY-15594A
    Phen-DC3 Trifluoromethanesulfonate
    Inhibitor 99.53%
    Phen-DC3 Trifluoromethanesulfonate is a G-quadruplex (G4) specific ligand which can inhibit FANCJ and DinG helicases with IC50s of 65±6 and 50±10 nM, respectively.
  • HY-112680A
    Carboxy pyridostatin trifluoroacetate salt
    Inhibitor ≥99.0%
    Carboxy pyridostatin trifluoroacetate salt has the peculiarity to exhibit high molecular specificity for RNA over DNA G4s.
  • HY-15595A
    360A iodide
    Activator ≥98.0%
    360A iodide is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.
  • HY-16967
    MM41
    Inhibitor 99.92%
    MM41 is a potent stabilizer of human telomeric and gene promoter DNA quadruplexes. MM41 is potently against the MIA PaCa-2 pancreatic cancer cell line with IC50 value of <10 nM.
  • HY-148012
    SOP1812
    SOP1812 is a naphthalene diimide (ND) derivative with anti-tumor activity. SOP1812 binds to quadruplex arrangements (G4s), and down-regulates several cancer gene pathways. SOP1812 shows great affinity to hTERT G4 and HuTel21 G4 with KD values of 4.9 and 28.4 nM, respectively. SOP1812 can be used for the research of cancer.
  • 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.
  • HY-135776
    BMVC2
    BMVC2 (o-BMVC) is a bisubstitute carbazole derivative of BMVC. BMVC2 is a G-quadruplex (G4) stabilizer.
  • HY-15176
    Pyridostatin
    Activator
    Pyridostatin (RR82) is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets the proto-oncogene Src. Pyridostatin reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells.
  • HY-15176B
    Pyridostatin TFA
    Activator
    Pyridostatin (RR82) TFA is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin TFA promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin TFA targets the proto-oncogene Src. Pyridostatin TFA reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells.
  • HY-135775
    BMVC
    BMVC is a potent G-quadruplex (G4) stabilizer and a selective telomerase inhibitor with an IC50 of ~0.2 μM. BMVC inhibits Taq DNA polymerase with an IC50 of ~2.5 μM. BMVC increases the melting temperature of G4 structure of telomere and accelerates telomere length shortening. Anticancer activities.
  • HY-133821
    N-Methylmesoporphyrin IX
    N-Methylmesoporphyrin IX (NMM), a widely used G-quadruplex DNA specific fluorescent binder, is an efficient probe for monitoring Aβ fibrillation. N-Methylmesoporphyrin IX is an in situ inhibitor and an ex situ monitor for Aβ amyloidogenesis both in vitro and in cells. N-Methylmesoporphyrin IX is sensitive to G-quadruplexes DNA but has no response to duplexes, triplexes and single-stranded forms DNA. N-Methylmesoporphyrin IX is nonfluorescent alone or in monomeric Aβ environments, but emits strong fluorescence through stacking with the Aβ assemblies.
  • HY-144712
    L5-DA
    L5-DA is a G-quadruplex (G4) ligand and selectively stabilized for G4s over ds26. L5-DA exhibits significant cytotoxicity against HeLa cells (IC50=4.3 μM). L5-DA stabilizes G4s in HeLa cells, induces apoptosis, and cell cycle arrest.
  • 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.