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

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

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

Target DNA/RNA Synthesis G-quadruplex Flavivirus Src Virus Protease

Research area Cancer

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Data Sheet SDS COA

Pyridostatin TFA structure

CAS No.: 1472611-44-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 450.00	BP-02314B-100mg	In stock	Get quote
250 mg	USD 798.00	BP-02314B-250mg	In stock	Get quote
500 mg	USD 1,388.00	BP-02314B-500mg	In stock	Get quote
1 g	USD 2,188.00	BP-02314B-1g	In stock	Get quote
2 g	Inquire	BP-02314B-2g	In stock	Inquire

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Description

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

Biological activity

Pyridostatin Trifluoroacetate Salt is a G-quadruplexe stabilizer, with a Kd of 490 nM. Pyridostatin stabilizes G-quadruplexes (G4s) in cells and elicits a DNA damage response by causing the formation of DNA double strand breaks (DSB). Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets gene bodies containing clusters of sequences with a propensity for G-quadruplex formation. 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.

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.C(=O)(C(F)(F)F)O
InChIKey: SLFYRKZWSPFGQZ-UHFFFAOYSA-N

Specifications

MW (average): 710.6597
Formula: C₃₃H₃₃F₃N₈O₇
CAS No.: 1472611-44-1
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 : 100 mg/mL

Documents

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.

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