Pyridostatin  (Synonyms: RR82)

Pyridostatin (RR82) is a G-quadruplex DNA stabilizing agent (K_d=490 nM). Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets the proto-oncogene Src. Pyridostatin reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells^[1][2].

Kd: 490 nM (G-quadruplexe)^[1]

Pyridostatin (RR82) (10 μM; 48 hours) induces cell cycle arrest^[1].
Pyridostatin is a very selective G-quadruplex DNA-binding small molecule designed to form a complex with and stabilize G-quadruplex structure. Pyridostatin causes neurite retraction, synaptic loss, and dose-dependent neuronal death. In cultured primary neurons, Pyridostatin induces the formation of DNA DSBs. Remarkably, Pyridostatin (1-5 μM, overnight) downregulates the BRCA1 protein, a protein that guards and repairs the neuronal genome, at the transcriptional level^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

596.64

C₃₁H₃₂N₈O₅

1085412-37-8

O=C(C1=CC(OCCN)=CC(C(NC2=NC3=C(C(OCCN)=C2)C=CC=C3)=O)=N1)NC4=CC(OCCN)=C5C=CC=CC5=N4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Rodriguez R, et al. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012;8(3):301-310. Published 2012 Feb 5.  [Content Brief]

  [2]. Koirala D, et al. A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Nat Chem. 2011;3(10):782-787. Published 2011 Aug 28.  [Content Brief]

  [3]. Moruno-Manchon JF, Koellhoffer EC, Gopakumar J, et al. The G-quadruplex DNA stabilizing drug pyridostatin promotes DNA damage and downregulates transcription of Brca1 in neurons. Aging (Albany NY). 2017;9(9):1957-1970.  [Content Brief]