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编 号:F031128
分子式:C31H32N8O5
分子量:596.64
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生物活性:
Pyridostatin (RR82) is a G-quadruplex DNA stabilizing agent (Kd=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.

体外研究:
Pyridostatin (RR82) (10 μM; 48 hours) induces cell cycle arrest. 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.
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