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 (23):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15176A
    Pyridostatin hydrochloride
    Inducer 98.53%
    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.
    Pyridostatin hydrochloride
  • HY-112680A
    Carboxy pyridostatin trifluoroacetate salt
    Inhibitor 99.13%
    Carboxy pyridostatin trifluoroacetate salt has the peculiarity to exhibit high molecular specificity for RNA over DNA G4s.
    Carboxy pyridostatin trifluoroacetate salt
  • HY-108477
    TMPyP4 tosylate
    Inhibitor ≥98.0%
    TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand. TMPyP4 tosylate inhibits the interaction between G-quadruplexes and IGF-1. TMPyP4 tosylate is a telomerase inhibitor and inhibits cancer cells proliferation. TMPyP4 tosylate is also a stabilizer of nucleic acid secondary structure and an acetylcholinesterase inhibitor. Besides, TMPyP4 tosylate has antiviral activity against SARS-CoV-2.
    TMPyP4 tosylate
  • HY-15594A
    Phen-DC3 Trifluoromethanesulfonate
    Inhibitor 98.99%
    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.
    Phen-DC3 Trifluoromethanesulfonate
  • 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.
    360A iodide
  • 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
  • HY-148012
    SOP1812
    98.37%
    SOP1812 (QN-302) 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.
    SOP1812
  • HY-15794
    Nemorubicin
    Nemorubicin (Methoxymorpholinyl doxorubicin) 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
  • 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.
    N-Methylmesoporphyrin IX
  • HY-135009
    2-Di-1-ASP
    99.97%
    2-Di-1-ASP (DASPI; Compound 18a) is a mono-stryryl dye, and widely used as mitochondrial stain and groove-binding fluorescent probes for double-stranded DNA. 2-Di-1-ASP is selective for G-quadruplex (G4) and double-stranded DNA.
    2-Di-1-ASP
  • HY-135775
    BMVC
    99.92%
    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.
    BMVC
  • HY-135776
    BMVC2
    99.89%
    BMVC2 (o-BMVC) is a bisubstitute carbazole derivative of BMVC. BMVC2 is a G-quadruplex (G4) stabilizer.
    BMVC2
  • 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.
    MM41
  • HY-148953
    MTR-106
    Modulator 99.40%
    MTR-106 is a potent and orally active G-quadruplex stabilizer and RNA polymerase I inhibitor. MTR-106 induces apoptosis and inhibits cell growth. MTR-106 can be used in research of cancer.
    MTR-106
  • 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.
    Pyridostatin
  • 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-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.
    Pyridostatin TFA
  • 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