|4-(2-氨基乙氧基)-N2,N6-双(4-(2-氨基乙氧基)喹啉-2-基)吡啶-2,6-二甲酰胺 2,2,2-三氟乙酸盐|CsnPharm

CAS No.: 1472611-44-1

Pyridostatin TFA/吡咯他汀（RR82）三氟乙酸盐 Catalog No. CSN19260

Synonyms: RR82 TFA;Pyridostatin Trifluoroacetate Salt;Pyridostatin (trifluoroacetate salt)

Pyridostatin Trifluoroacetate stabilizes and binds G-quadruplexe with Kd of 490 nM (cell-free assay), which targets the proto-oncogene c-kit, K-ras and Bcl-2.

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技术信息

生物活性

描述Pyridostatin is a highly selective G-quadruplex binding small molecule that promotes the folding of telomeric G-quadruplexes. The K_d vaule of pyridostatin for G-quadruplex is 490 ± 80nM^[3]. Treatment with 2μM pyridostatin for 24 hours induces DNA damage and cell cycle arrest in MRC5-SV40 cells. Pre-treating EdU negative G1 and G2 cells with the transcription inhibitor DRB prevented pyridostatin (20μM) from inducing γH2AX foci. Pyridostatin predominantly interacts with non-telomeric DNA loci at low concentrations. Pyridostatin (2μM) downregulated the expression of SRC and reduced SRC-dependent cell motility in MRC5-SV40 cells after 24 hours of treatment^[4].
参考文献

[1] Murat P, Zhong J, et al. G-quadruplexes regulate Epstein-Barr virus-encoded nuclear antigen 1 mRNA translation. Nat Chem Biol. 2014 May;10(5):358-64.
[2] 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.
[3] Koirala D, Dhakal S, Ashbridge B, Sannohe Y, Rodriguez R, Sugiyama H, Balasubramanian S, Mao H. A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Nat Chem. 2011 Aug 28;3(10):782-7.
[4] Rodriguez R, Miller KM, Forment JV, Bradshaw CR, Nikan M, Britton S, Oelschlaegel T, Xhemalce B, Balasubramanian S, Jackson SP. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012 Feb 5;8(3):301-10.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.4071 mL
- 7.0357 mL
- 14.0714 mL
- 5 mM
- 0.2814 mL
- 1.4071 mL
- 2.8143 mL
- 10 mM
- 0.1407 mL
- 0.7036 mL
- 1.4071 mL

技术信息

CAS号

1472611-44-1

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C33H33F3N8O7

运输

蓝冰

分子量

710.66

别名

RR82 TFA;Pyridostatin Trifluoroacetate Salt;Pyridostatin (trifluoroacetate salt);Pyridostatin;PDS

溶解度

DMSO	430.0 mg/mL (605.1 mM)
Water	170.0 mg/mL (239.2 mM)

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Pyridostatin TFA/吡咯他汀（RR82）三氟乙酸盐 Catalog No. CSN19260

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