G-quadruplex

G-quadruplex ligands bind four-stranded structures that form in guanine-rich DNA and RNA sequences. Four guanines pair through Hoogsteen hydrogen bonds into a planar G-quartet, and stacked quartets are stabilized by potassium ions. Parallel four-stranded complexes of guanine-rich DNA were described in 1988. In 2013 a structure-specific antibody visualized G-quadruplexes in human cell nuclei, with numbers that changed during the cell cycle. Such structures occur at telomeres, in gene promoters and in ribosomal DNA. Pyridostatin, reported in 2008, stabilizes telomeric G-quadruplexes and triggers a DNA damage response there. 360A and MTR-106 are further stabilizing ligands, and BMVC-8C3O is a carbazole-based G-quadruplex ligand. Quarfloxin targets G-quadruplexes in ribosomal DNA and inhibits ribosomal RNA (rRNA) biogenesis.

11 Items

  • Quarfloxin
    Cat. No.
    A12380

    Quarfloxin (CX-3543)

    Synonyms: CX 3543; Quarfloxacin

    Quarfloxin (CX-3543) is a fluoroquinolone derivative with antineoplastic activity. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template, a critical interaction for rRNA biogenesis that is overexpressed in cancer cells; disruption of this G-quadruplex DNA:protein interaction in aberrant rRNA biogenesis may result in the inhibition of ribosome synthesis and tumor cell apoptosis.

    1 mg
    $115.00
    5 mg
    $175.00
    All 7 sizes
  • Pyridostatin TFA salt
    Cat. No.
    A22462

    Pyridostatin TFA salt

    Synonyms: Pyridostatin; PDS

    Pyridostatin stabilizes G-quadruplexes (G4s) in cells and elicits a DNA damage response by causing the formation of DNA double strand breaks (DSB).

    1 mg
    $25.00
    5 mg
    $65.00
    All 7 sizes
  • 360A
    Cat. No.
    A14975

    360A

    360A is a strong affinity and selectivity inhibitor of G-quadruplex structures.

    1 mg
    $90.00
    2 mg
    $145.00
    All 7 sizes
  • 360A iodide
    Cat. No.
    A14976

    360A iodide

    360A is a strong affinity and selectivity inhibitor of G-quadruplex structures.

    5 mg
    $195.00
    10 mg
    $315.00
    All 4 sizes
  • L5-DA
    Cat. No.
    A30774

    L5-DA

    L5-DA is a selective G-quadruplex stabilizer that preferentially interacts with G4 structures over double-stranded DNA. This compound exhibits notable cytotoxicity against HeLa cells, with an IC50 value of 4.3 μM. L5-DA effectively stabilizes G4s within HeLa cells, leading to the induction of apoptosis and cell cycle arrest. Its role in modulating G-quadruplexes makes it a valuable tool for research in cancer biology and therapeutic development.

    1 mg
    $375.00
    5 mg
    $965.00
    All 3 sizes
  • MTR-106
    Cat. No.
    A30807

    MTR-106

    MTR-106 is a potent G-quadruplex stabilizer that also functions as an RNA polymerase I inhibitor. This compound has demonstrated the ability to induce apoptosis and inhibit cell proliferation, making it a valuable tool in cancer research. Its unique mechanism of action provides insights into G-quadruplex dynamics and their implications in tumor biology.

    1 mg
    $85.00
    5 mg
    $175.00
    All 6 sizes
  • Y502-2304
    Cat. No.
    A32290

    Y502-2304

    Y502-2304 is a potent c-Myc G-quadruplex stabilizer that exhibits significant antiproliferative activity in multiple myeloma (MM) cells. It effectively downregulates both c-Myc mRNA and protein expression, leading to the induction of apoptosis characterized by increased γH2AX levels and elevated reactive oxygen species (ROS). Additionally, Y502-2304 disrupts mitochondrial function and demonstrates a marked inhibition of tumor growth in xenograft models of MM. This compound is suitable for various research applications focused on elucidating the molecular mechanisms underlying multiple myeloma.

    Out of stock

    All 3 sizes
  • Phen-DC3 Trifluoromethanesulfonate
    Cat. No.
    A54683

    Phen-DC3 Trifluoromethanesulfonate

    Synonyms: Phen-DC3 Triflate

    Phen-DC3 Trifluoromethanesulfonate is a specific ligand that targets G-quadruplex (G4) structures, effectively inhibiting the helicases FANCJ and DinG with IC50 values of 65±6 nM and 50±10 nM, respectively. This compound plays a critical role in research focused on telomere biology, DNA replication, and cancer therapeutics. Its ability to modulate G4 structures makes it a valuable tool for investigating G4-associated cellular processes and the development of novel anti-cancer strategies.

    1 mg
    $40.00
    5 mg
    $85.00
    All 6 sizes
  • BMVC2
    Cat. No.
    A54686

    BMVC2

    Synonyms: o-BMVC

    BMVC2 is a bisubstituted carbazole derivative that serves as a G-quadruplex (G4) stabilizer. This compound promotes the formation and stabilization of G-quadruplex structures, which are important in the regulation of gene expression and telomere maintenance. BMVC2 is utilized in research applications focusing on cancer biology, antiviral therapies, and the development of novel molecular therapeutics targeting G4 DNA structures.

    5 mg
    $195.00
    10 mg
    $320.00
    All 5 sizes
  • Pyridostatin trihydrochloride
    Cat. No.
    A54689

    Pyridostatin trihydrochloride

    Synonyms: RR82 trihydrochloride

    Pyridostatin trihydrochloride is a potent G-quadruplex stabilizer with a binding affinity (Kd) of 490 nM, effectively targeting DNA and RNA G-quadruplex structures within cellular environments. This compound induces growth arrest in human cancer cells through mechanisms involving replication- and transcription-dependent DNA damage. Pyridostatin specifically impacts the proto-oncogene Src, leading to diminished SRC protein levels and reduced SRC-dependent cellular motility in human breast cancer cells. Its applications extend to cancer research, particularly in studying mechanisms of tumor progression and drug resistance.

    1 mg
    $30.00
    2 mg
    $40.00
    All 7 sizes

11 Items

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