Pyridostatin(Synonyms: RR82)

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Pyridostatin (Synonyms: RR82)

Pyridostatin (RR82) 是一种高选择性的 G-quadruplex DNA 稳定剂 (Kd=490 nM)。Pyridostatin 通过诱导复制和转录依赖的 DNA 损伤促进人类癌细胞生长停滞。Pyridostatin 靶向原癌基因 Src。Pyridostatin 降低人乳腺癌细胞 SRC 蛋白水平和 SRC 依赖的细胞运动。

Pyridostatin(Synonyms: RR82)

Pyridostatin Chemical Structure

CAS No. : 1085412-37-8

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Pyridostatin 的其他形式现货产品:

Pyridostatin hydrochloride

生物活性

Pyridostatin (RR82) is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets the proto-oncogene Src. Pyridostatin reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells[1][2].

IC50 & Target

Kd: 490 nM (G-quadruplexe)[1]
体外研究
(In Vitro)

Pyridostatin (RR82) (10 μM; 48 hours) induces cell cycle arrest[1].
Pyridostatin is a very selective G-quadruplex DNA-binding small molecule designed to form a complex with and stabilize G-quadruplex structure. Pyridostatin causes neurite retraction, synaptic loss, and dose-dependent neuronal death. In cultured primary neurons, Pyridostatin induces the formation of DNA DSBs. Remarkably, Pyridostatin (1-5 μM, overnight) downregulates the BRCA1 protein, a protein that guards and repairs the neuronal genome, at the transcriptional level[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Over 60 different cancer cell lines
Concentration: 10 μM
Incubation Time: 48 hours
Result: Predominantly accumulated in the G2 phase of the cell cycle over 60 different cancer cell lines.

分子量

596.64

Formula

C31H32N8O5
CAS 号

1085412-37-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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, Koellhoffer EC, Gopakumar J, 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.

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