BiochemProbe — Life Science Research Reagents

Pyridostatin hydrochloride salt form · hydrochloride · Parent Pyridostain · Synonyms: RR82 hydrochloride

Pyridostatin (RR82) hydrochloride is a G-quadruplex DNA stabilizing agent (Kd=490 nM).

For research use only. Not for human or veterinary use.

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Description

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

Biological activity

Pyridostatin (2 μM; 72 h) hydrochloride potently inhibits the proliferation of SV40-transformed human MRC5 fibroblasts. Pyridostatin (2 μM; 1-10 days) hydrochloride induces G2-phase cell cycle arrest and activates the DNA damage response in SV40-transformed human MRC5 fibroblasts and various human cancer cell lines. Long-term treatment causes G1-phase arrest in some cells, and checkpoint inhibition reverses this cell cycle arrest.

Identifiers

SMILES
C1=CC=C2C(=C1)C(=CC(=N2)NC(=O)C3=CC(=CC(=N3)C(=O)NC4=NC5=CC=CC=C5C(=C4)OCCN)OCCN)OCCN.Cl.Cl.Cl.Cl.Cl
InChIKey
SRIZPFGTXSQRFM-UHFFFAOYSA-N

Specifications

MW (average)
778.9410
Formula
C31H37Cl5N8O5
CAS No.
1781882-65-2
Physical state
Solid
Color
White to off-white
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
4°C, sealed storage, away from moisture

Solubility

Soluble in H2O

In vitro
H2O : 50 mg/mL

References

[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.
[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.
[3]. 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;9(9):1957-1970.
[4]. Zhang X, et al. Chemical profiling of DNA G-quadruplex-interacting proteins in live cells. Nat Chem. 2021 Jul;13(7):626-633.

Same research area

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