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

G-quadruplex

G-quadruplex

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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-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-181850
    Telomeric G4s ligand 2
    		Ligand
    Telomeric G4s ligand 2 is an orally active, selective ligand of telomeric G-quadruplex (G4), with an IC50 of 0.4 μM. Telomeric G4s ligand 2 binds to dimeric telomeric G4, inhibits the activities of DHX36 and BLM helicases. Telomeric G4s ligand 2 activates cGAS-STING and TERRA-ZBP1 pathways, inducing autophagy and G2/M cell cycle arrest, and exhibits antiproliferative effects across cancer cell lines. Telomeric G4s ligand 2 can be used for the study of colorectal cancer.
    Telomeric G4s ligand 2
  • 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-182029
    G-quadruplex ligand 5
    		Ligand
    G-quadruplex ligand 5 is a G-quadruplex (G4) ligand. G-quadruplex ligand 5 selectively stabilizes cancer-associated G4 oligonucleotides and shows cytotoxicity toward cancer cells. G-quadruplex ligand 5 can be used for the research of cancer.
    G-quadruplex ligand 5
  • 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-170814
    G-quadruplex ligand 3
    		Ligand
    G-quadruplex ligand 3 (Compound 16) is a G-quadruplex ligand with anticancer effects that chelate iron. G-quadruplex ligand 3 stabilizes G-quadruplexes in human leukemia Jurkat cells. G-quadruplex ligand 3 localizes in the cell nucleus, serving as a fluorescent nuclear tracer for the labile iron pool.
    G-quadruplex ligand 3
  • 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-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-181713
    Antibiofilm agent-19
    		Modulator
    Antibiofilm agent-19 is an antibiofilm agent with iron-chelating activity. Antibiofilm agent-19 potently inhibits biofilm formation by wild-type PAO1 and the hyper-biofilm mutant strain PAO1-ΔwspF. Antibiofilm agent-19 promotes the formation of c-di-GMP G-quadruplexes and disrupts iron acquisition systems. It can be used in studies on antibacterial adjuvants.
    Antibiofilm agent-19
  • 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