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[1][2].
Nemorubicin is a derivative of doxorubicin, and has antitumor activity.
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[1].
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.
Pyridostatin (RR82) TFA is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin TFA promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin TFA targets the proto-oncogene Src. Pyridostatin TFA reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells[1][2][3].
APTO-253 is an inducer of Kruppel-like factor 4 (KLF4), and also stabilizes Gquadruplex, with anti-proliferative activity.
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.
SOP1812 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[1].
Pyridostatin is a G-quadruplexe stabilizer, with a Kd of 490 nM.
BMVC2 (o-BMVC) is a bisubstitute carbazole derivative of BMVC. BMVC2 is a G-quadruplex (G4) stabilizer[1].
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[1].
Pyridostatin hydrochloride is a G-quadruplexe stabilizer, with a Kd of 490 nM.
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[1].
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.
TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand, which inhibits the interaction between G-quadruplexes and IGF-1[1]. TMPyP4 tosylate (TMP 1363) is a telomerase inhibitor with antitumor effects in osteosarcoma cell lines[2].