Pyridostatin (trifluoroacetate salt) (Synonyms: RR82 TFA) |
| Katalog-Nr.GC48016 |
Pyridostatin (RR82) TFA ist ein G-Quadruplex-DNA-Stabilisierungsmittel (Kd = 490 nM). Pyridostatin (Trifluoracetatsalz) fÖrdert den Wachstumsstillstand in menschlichen Krebszellen, indem es replikations- und transkriptionsabhÄngige DNA-SchÄden induziert. Pyridostatin (Trifluoracetatsalz) zielt auf das Proto-Onkogen Src ab. Pyridostatin (Trifluoracetatsalz) reduzierte die SRC-Proteinspiegel und die SRC-abhÄngige ZellmotilitÄt in menschlichen Brustkrebszellen.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1472611-44-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Pyridostatin (trifluoroacetate salt) is a highly selective G-quadruplex-binding small molecule that was designed to target polymorphic G-quadruplex structures regardless of sequence variability. As a highly selective G-quadruplex DNA stabilizer,Kd is 490 nM. Pyridostatin has anti-proliferative effects and induces telomere dysfunction[1-4].
Pyridostatin(2 µM pyridostatin;24 h) induced DNA damage and checkpoint-dependent cell-cycle arrest in MRC-5 SV40 cells[5]. Pyridostatin(0.01-5 µM pyridostatin;24-96 h) induced neurotoxicity and promoted the formation of DNA double-strand breaks (DSBs) in cultured neurons[6]. Pyridostatin(10 µM pyridostatin;24 h) significantly downregulated 22 proteins but upregulated 16 proteins in HeLa cancer cells, of which the genes both contain a number of G4 potential sequences, Pyridostatin regulation on gene expression is far more complicated than inducing/stabilizing G4 structures[7].
References:
[1]. Rodriguez R, MÜller S, et,al. A novel small molecule that alters shelterin integrity and triggers a DNA-damage response at telomeres. J Am Chem Soc. 2008 Nov 26;130(47):15758-9. doi: 10.1021/ja805615w. PMID: 18975896; PMCID: PMC2746963.
[2]. Patel DJ, Phan AT, et,al. Human telomere, oncogenic promoter and 5'-UTR G-quadruplexes: diverse higher order DNA and RNA targets for cancer therapeutics. Nucleic Acids Res. 2007;35(22):7429-55. doi: 10.1093/nar/gkm711. Epub 2007 Oct 2. PMID: 17913750; PMCID: PMC2190718.
[3]. MÜller S, Kumari S, et,al. Small-molecule-mediated G-quadruplex isolation from human cells. Nat Chem. 2010 Dec;2(12):1095-8. doi: 10.1038/nchem.842. Epub 2010 Oct 10. PMID: 21107376; PMCID: PMC3119466.
[4]. Koirala D, Dhakal S, 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. doi: 10.1038/nchem.1126. PMID: 21941250; PMCID: PMC3277938.
[5]. Rodriguez R, Miller KM, et,al. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012 Feb 5;8(3):301-10. doi: 10.1038/nchembio.780. PMID: 22306580; PMCID: PMC3433707.
[6]. 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. doi: 10.18632/aging.101282. PMID: 28904242; PMCID: PMC5636668.
[7]. Hou Y, Gan T, et,al. G-quadruplex inducer/stabilizer pyridostatin targets SUB1 to promote cytotoxicity of a transplatinum complex. Nucleic Acids Res. 2022 Apr 8;50(6):3070-3082. doi: 10.1093/nar/gkac151. PMID: 35258624; PMCID: PMC8989551.
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *