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Pyridostatin hydrochloride

Names

[ CAS No. ]:
1781882-65-2

[ Name ]:
Pyridostatin hydrochloride

Biological Activity

[Description]:

Pyridostatin hydrochloride is a G-quadruplexe stabilizer, with a Kd of 490 nM.

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> G-quadruplex
Research Areas >> Cancer

[Target]

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


[In Vitro]

Pyridostatin hydrochloride is a G-quadruplexe stabilizer, with a Kd of 490 nM[1]. Pyridostatin (PDS) shows neurotoxic activity against primary cortical neurons at 0.01-5 μM, causes DNA double-strand breaks (DSBs) at 1 μM, downregulates BRCA1 in neurons at 1, 2 or 5 μM[2]. Pyridostatin interacts with G-quadruplex motifs in SRC and alters mRNA levels of damaged genes[3].

[Cell Assay]

Cells are plated at equal confluence and either untreated or treated with 2 μM Pyridostatin continually for 72 h. Cells from individual plates are trypsinized and counted in a Coultercounter. Graphs represent total cell numbers at each time interval and error bars represent S.E.M. Data represent three independent experiments[3].

[References]

[1]. Koirala D, et al. A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Nat Chem. 2011 Aug 28;3(10):782-7.

[2]. Moruno-Manchon JF, et al. The G-quadruplex DNA stabilizing drug pyridostatin promotes DNA damage and downregulates transcription of Brca1 in neurons. Aging (Albany NY). 2017 Sep 12;9(9):1957-1970.

[3]. Rodriguez R, et al. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012 Feb 5;8(3):301-10.


[Related Small Molecules]

APTO-253 | Phen-DC3 Trifluoromethanesulfonate | 360A iodide | Pyridostatin

Chemical & Physical Properties

[ Molecular Formula ]:
C31H37Cl5N8O5

[ Molecular Weight ]:
778.94

[ Storage condition ]:
2-8℃

Related Compounds