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 (51):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15176A
    Pyridostatin hydrochloride
    Inducer 99.95%
    Pyridostatin (RR82) hydrochloride is a G-quadruplex DNA stabilizing agent (Kd=490 nM) and can target DNA and RNA G4s in cells. 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-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 98.64%
    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-112680A
    Carboxy pyridostatin trifluoroacetate salt
    99.49%
    Carboxy pyridostatin trifluoroacetate salt is a G-quadruplex ligand. Carboxy pyridostatin trifluoroacetate salt has a highly molecular specificity to RNA on DNA G4s and reduces ATF-5 protein. Carboxy pyridostatin trifluoroacetate salt reduces cell proliferation and hinders stress granule (SG) formation.
    Carboxy pyridostatin trifluoroacetate salt
  • HY-133821
    N-Methylmesoporphyrin IX
    99.65%
    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-179480
    G-quadruplex ligand 4
    Ligand
    G-quadruplex ligand 4 is a chromenone derivative and is a human telomerase reverse transcriptase (hTERT) G4 ligand. G-quadruplex ligand 4 downregulates hTERT expression and exhibits notable cytotoxicity towards triple-negative breast cancer (TNBC) cell lines. G-quadruplex ligand 4 can cause S/G2 cell cycle arrest and induce apoptosis. G-quadruplex ligand 4 downregulates the expression of hTERT, KRAS, and BCL-2. G-quadruplex ligand 4 can be used for the research of TNBC.
    G-quadruplex ligand 4
  • HY-182055
    Anticancer agent 309
    Activator
    Anticancer agent 309 (Compound HZ-1) is an anticancer agent and G-quadruplex binder, with Kd values of 2.46 μM and 1.61 μM for c-Myc G4 and KRAS G4, respectively. Anticancer agent 309 promotes the formation of intranuclear G4. Anticancer agent 309 shows higher selectivity for parallel G4 than for non-parallel G4. Anticancer agent 309 inhibits the NRF2 signaling pathway and reduces the expression of XCT and GPX4. Anticancer agent 309 induces Ferroptosis, Apoptosis and immunogenic cell death in cells. Anticancer agent 309 exerts antitumor efficacy against breast cancer. Anticancer agent 309 is applicable for the research of breast cancer.
    Anticancer agent 309
  • HY-183984
    G-quadruplex ligand 6
    Ligand
    G-quadruplex ligand 6 is a G-quadruplex ligand targeting the c-MYC promoter with anti-tumor activity. G-quadruplex ligand 6 forms a non-covalent complex with Pu22, a G-quadruplex model of the c-MYC promoter, with a microscopic dissociation constant Kd of 0.202 μM. G-quadruplex ligand 6 selectively inhibits tumor cell proliferation, blocks the binding of transcription factors by stabilizing the G-quadruplex in the c-MYC promoter, and thereby regulates the expression of proto-oncogenes. G-quadruplex ligand 6 can be used in the research of pancreatic cancer, non-small cell lung cancer, colorectal cancer, and triple-negative breast cancer.
    G-quadruplex ligand 6
  • HY-164421
    PhpC
    Modulator 98.90%
    PhpC is a G-quadruplex (G4)-DNA/RNA disruptor. PhpC disrupts DNA and RNA G4 structures and promotes G4 helicase activity. PhpC effectively enhancing the activity of Taq polymerase. PhpC modulates G-quadruplexs (G4s) both in vitro and in cells.
    PhpC
  • HY-15523
    Braco-19
    98.01%
    Braco-19 is a potent telomerase/telomere inhibitor, preventing the capping and catalytic action of telomerase. Braco-19 acts as G-quadruplex (GQ) binding ligand, stabilizing G-quadruplexes formation at the 3V telomeric DNA overhang and produce rapid senescence or selective cell death. Braco-19 is also a HAdV virus replication inhibitor.
    Braco-19
  • HY-148012
    SOP1812
    98.46%
    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-15176B
    Pyridostatin TFA
    Inducer 99.17%
    Pyridostatin (RR82) TFA is a G-quadruplex (G4) inducer/stabilizer with a Kd of 490 nM. Pyridostatin TFA also acts as an inhibitor of Zika virus (ZIKV) NS2B-NS3 protease, with an IC50 of 11.0 μM. Pyridostatin TFA interacts with G-quadruplex structures, regulates the expression of SRC and SUB1, and induces replication- and transcription-dependent DNA damage, growth arrest, and genomic instability. Pyridostatin TFA exhibits antiproliferative and antiviral activities. Pyridostatin TFA can be used in studies related to breast cancer, cervical cancer, and Zika virus infection.
    Pyridostatin TFA
  • 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-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-135775
    BMVC
    98.40%
    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-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-15176
    Pyridostatin
    Activator
    Pyridostatin (RR82) is a G-quadruplex DNA stabilizing agent (Kd=490 nM) and can target DNA and RNA G4s in cells. 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-DY1075
    N-Methylmesoporphyrin IX (solution)
    N-Methylmesoporphyrin IX (NMM) (solution) , 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.
    Solvent and concentration: DMSO: 2 mM
    N-Methylmesoporphyrin IX (solution)
  • HY-112680
    Carboxypyridostatin
    99.41%
    Carboxypyridostatin is a G-quadruplex ligand. Carboxypyridostatin has a highly molecular specificity to RNA on DNA G4s and reduces ATF-5 protein. Carboxypyridostatin reduces cell proliferation and hinders stress granule (SG) formation.
    Carboxypyridostatin
  • HY-15176C
    Pyridostatin trihydrochloride
    Inducer 99.85%
    Pyridostatin (RR82) trihydrochloride is a G-quadruplex (G4) inducer/stabilizer with a Kd of 490 nM. Pyridostatin trihydrochloride also acts as an inhibitor of Zika virus (ZIKV) NS2B-NS3 protease, with an IC50 of 11.0 μM. Pyridostatin trihydrochloride interacts with G-quadruplex structures, regulates the expression of SRC and SUB1, and induces replication- and transcription-dependent DNA damage, growth arrest, and genomic instability. Pyridostatin trihydrochloride exhibits antiproliferative and antiviral activities. Pyridostatin trihydrochloride can be used in studies related to breast cancer, cervical cancer, and Zika virus infection.
    Pyridostatin trihydrochloride