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Pyridostatin

Names

[ CAS No. ]:
1085412-37-8

[ Name ]:
Pyridostatin

[Synonym ]:
2,6-Pyridinedicarboxamide, 4-(2-aminoethoxy)-N,N-bis[4-(2-aminoethoxy)-2-quinolinyl]-
4-(2-Aminoethoxy)-N,N'-bis[4-(2-aminoethoxy)-2-quinolinyl]-2,6-pyridinedicarboxamide
RR82
Pyridostatin
Pyridostatin trifluoroacetate salt

Biological Activity

[Description]:

Pyridostatin 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 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 | Pyridostatin hydrochloride | Phen-DC3 Trifluoromethanesulfonate | 360A iodide

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
753.8±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C31H32N8O5

[ Molecular Weight ]:
596.636

[ Flash Point ]:
409.7±32.9 °C

[ Exact Mass ]:
596.249573

[ PSA ]:
202.62000

[ LogP ]:
0.59

[ Vapour Pressure ]:
0.0±2.5 mmHg at 25°C

[ Index of Refraction ]:
1.726

Related Compounds