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-144712
    L5-DA
    		99.03%
    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.
    L5-DA
  • HY-145748
    SYUIQ-5
    		Ligand 99.03%
    SYUIQ-5 is a G-quadruplex ligand. SYUIQ-5 stabilizes G-quadruplex and induce senescence. SYUIQ-5 inhibits c-myc gene promoter activity. SYUIQ-5 induces cancer cells autophagy by triggering telomere damage through TRF2 delocalization from telomeres.
    SYUIQ-5
  • HY-16967
    MM41
    		Ligand 98.89%
    MM41 is a quadruplex-interacting compound. MM41 binds tightly to quadruplexes encoded in the promoter sequences of the BCL-2 and k-RAS genes. MM41 reduces BCL-2 and k-RAS protein levels, increases caspase 3. MM41 has antitumor effects against pancreatic cancer.
    MM41
  • HY-148953
    MTR-106
    		Modulator 98.21%
    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-135776
    BMVC2
    		98.93%
    BMVC2 (o-BMVC) is a bisubstitute carbazole derivative of BMVC. BMVC2 is a G-quadruplex (G4) stabilizer.
    BMVC2
  • HY-W543137
    PT-ttpy
    		98.0%
    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-170643
    G4/hTERT-IN-4
    		Inhibitor 98.55%
    G4/hTERT-IN-4 (compound b4) is a potent inhibitor of G4/hTERT. G4/hTERT-IN-4 plays an important role in cancer research.
    G4/hTERT-IN-4
  • HY-162796
    TS-2
    		98.27%
    TS-2 is a fluorescent ligand of c-Myc G4 with anticancer activity. TS-2 inhibits the growth of cancer cells and induces apoptosis of cancer cells by targeting the c-MYC oncogene promoter G4, causing transcriptional repression of the c-Myc oncogene.
    TS-2
  • HY-164528
    SJ26
    		98.65%
    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-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-161693
    Telomeric G4s ligand 1
    		99.70%
    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-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-174384
    MET Transcription-IN-1
    		Ligand
    MET Transcription-IN-1 (Compound C3) is an orally active MET transcription inhibitor. MET Transcription-IN-1 can efficiently bind and stabilize the G-quadruplex in the MET promoter region, thereby inhibiting c-Met expression. MET Transcription-IN-1 can also overcome drug resistance caused by specific c-Met mutations. MET Transcription-IN-1 is capable of inhibiting tumor cell proliferation, migration, and invasion, as well as inducing cell cycle arrest and apoptosis. MET Transcription-IN-1 has antitumor activity, and can be used in the research of tumors such as non-small cell lung cancer.
    MET Transcription-IN-1
  • HY-182706
    NSC 373981
    		Inhibitor
    NSC 373981 is a CARD11 G4 stabilizer. NSC 373981 stabilizes the CARD11 G4 structure and inhibits CARD11 transcription in cells. NSC 373981 also inhibits BCL2 and MYC. NSC 373981 suppresses the transcription of KRAS and TERT. NSC 373981 exhibits anticancer activity against diffuse large B-cell lymphoma.
    NSC 373981
  • HY-183980
    MJ-NR-27
    MJ-NR-27 is a bifunctional small molecule of ribonuclease-targeting chimera (RIBOTAC) that targets NRAS mRNA containing a G-quadruplex structure. MJ-NR-27 uses RNase L ligand 3 (HY-177030) as the RNase L ligand, RNA binder 4 (HY-183981) as the RNA binder, and Bis-PEG3-acid (HY-126891) as the linker. MJ-NR-27 achieves target RNA degradation by recruiting ribonuclease RNase L, and significantly induces morphological changes in tumor cells. MJ-NR-27 can be used in cancer research.
    MJ-NR-27
  • 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-181284
    BYBC-1
    		Ligand
    BYBC‑1 is a selective G4‑RNA‑targeting ligand with high affinity forKRAS and NRAS G4‑RNAs (Kd = 0.05-0.28 μM). BYBC‑1 stabilizes G4‑RNA structures in KRAS and NRAS mRNA, blocks thePI3K/AKT and MAPK/ERK pathways, activates the DNA damage response (DDR), suppresses energy metabolism, and induces S‑phase arrest and apoptosis. BYBC‑1 exhibits high selectivity over non‑malignant fibroblasts and significantly inhibits the growth of HCT‑116 xenograft tumors in vivo. BYBC‑1 can be used for the study of colorectal cancer.
    BYBC-1
  • HY-D3415
    TOR-G4
    		Ligand
    TOR-G4 is a Fluorescent probe that binds to G-quadruplex (G4) nucleic acid structures. TOR-G4 exhibits a unique fluorescence lifetime when bound to G4 compared to other structures, enabling sensitive discrimination between G4-bound and non-G4-bound states. TOR-G4 mainly colocalizes with RNA in the cytoplasm and nucleolus. TOR-G4 can be used to investigate the roles of RNA G4 in cells. TOR-G4 shows cytotoxicity against osteosarcoma cells.
    TOR-G4
  • HY-P11486
    NOTA-RHAU18
    		Ligand
    NOTA-RHAU18 is a conjugate of the chelator NOTA and the peptide RHAU18. NOTA-RHAU18 can be used to synthesize the radiolabeled peptide probe [18F]AlF-NOTA-RHAU18. [18F]AlF-NOTA-RHAU18 targets mitochondrial DNA G4. [18F]AlF-NOTA-RHAU18 can be used to visualize and detect solid tumors in homozygous mice. [18F]AlF-NOTA-RHAU18 can also be used in PET imaging studies.
    NOTA-RHAU18