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.

4 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
  • 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
  • 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

4 Items

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