Pyridostatin

Pyridostatin (CAS 1085412-37-8) is a synthetic small molecule functioning as a stabilizer of G-quadruplex DNA structures. G-quadruplexes are secondary DNA structures enriched in guanine-rich regions, such as telomeres and promoter sequences of certain oncogenes (e.g., c-kit, K-ras, Bcl-2), affecting DNA replication, transcription regulation, and telomere integrity. Pyridostatin selectively binds and stabilizes these structures, leading to competitive inhibition of telomere-associated protein binding and subsequent induction of telomere dysfunction. In cellular assays, Pyridostatin selectively inhibits growth of various cancer cell lines (HeLa, U2OS, HT1080) with IC50 values ranging from 0.89 to 10 μM, demonstrating potential utility for cancer biology research.
References:
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[2] Müller S, Sanders D A, Di Antonio M, et al. Pyridostatin analogues promote telomere dysfunction and long-term growth inhibition in human cancer cells. Organic & biomolecular chemistry, 2012, 10(32): 6537-6546.
[3] McLuckie K I E, Di Antonio M, Zecchini H, et al. G-quadruplex DNA as a molecular target for induced synthetic lethality in cancer cells. Journal of the American Chemical Society, 2013, 135(26): 9640-9643.