PyrIDOSTATin TFA 是一种 G-四链体稳定剂，靶向原癌基因 Src，降低人乳腺癌细胞 Src 蛋白水平和 Src 依赖的细胞运动。它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 Trifluoroacetate Salt is a G-quadruplexe stabilizer with Kd of 490 nM in a cell-free assay, which targets a series of proto-oncogenes including c-kit, K-ras and Bcl-2.

Pyridostatin decreases the proliferation of MRC-5–SV40 cells and various cancer cell lines, and induces cell-cycle arrest by DNA-damage checkpoint activation. Pyridostatin also reduces SRC-dependent cell motility in MDA-MB-231 cells by interacting with G-quadruplex motifs in SRC.Pyridostatin decreases EBNA1 synthesis via inhibition of G-quadruplexes.

Cell lines: MRC-5–SV40 cells and various cancer cell linesConcentrations: 10 μMIncubation Time: 48 hMethod: Cells are plated at equal confluence and are left either untreated or were treated with 2 μM pyridostatin continually during the indicated time before harvesting the cells. Cells from individual plates are trypsinized and counted in a Coulter counter. Graphs represent the total cell numbers at each time interval, and the error bars represent the s.e.m. Data represent three independent experiments.

1472611-44-1

C37H35F9N8O11

938.718

DMSO:90 mg/mL (95.88 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years