Pyridostatin (hydrochloride)

Pyridostatin (RR82) hydrochloride is a G-quadruplex DNA stabilizing agent (K_d=490 nM) and can target DNA and RNA G4s in cells. Pyridostatin hydrochloride promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin hydrochloride targets the proto-oncogene Src. Pyridostatin hydrochloride reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells^[1][2]. IC50 & Target:Kd: 490 nM (G-quadruplexe)^[1] In Vitro:Pyridostatin (RR82) hydrochloride (10 μM; 48 hours) induces cell cycle arrest^[1].
Pyridostatin hydrochloride is a very selective G-quadruplex DNA-binding small molecule designed to form a complex with and stabilize G-quadruplex structure. Pyridostatin hydrochloride causes neurite retraction, synaptic loss, and dose-dependent neuronal death. In cultured primary neurons, Pyridostatin hydrochloride induces the formation of DNA DSBs. Remarkably, Pyridostatin hydrochloride (1-5 μM, overnight) downregulates the BRCA1 protein, a protein that guards and repairs the neuronal genome, at the transcriptional level^[3].