Uses
Pyridostatin hydrochloride has been used as a G-quadruplex (G4)-stabilizing ligand to check the effect of G4s on fork progression. It has also been used as a G4-stabilizing ligand to study the effect of G4 on apurinic/apyrimidinic endonuclease 1 (APE1) mediated Kirsten rat sarcoma virus (KRAS) expression in pancreatic ductal adenocarcinoma (PDAC) cell lines.
Biological Activity
Pyridostatin (RR82) hydrochloride is a highly selective G-quadruplex DNA stabilizer (Kd=490 nM). It promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage.
in vitro
Pyridostatin (RR82) hydrochloride (10 μM; 48 hours) induces cell cycle arrest. It is a very selective G-quadruplex DNA-binding small molecule designed to form a complex with and stabilize G-quadruplex structure.
target
Kd: 490 nM (G-quadruplexe)