AG490 inhibits the proliferation of K562 and down-regulates protein phosphatase PHLPP expression.
- Author:
Chao-Qi YAN
1
;
Li-Jun ZHANG
Author Information
1. Department of Hematology, First Affiliated Hospital of China Medical University, Shenyang, China.
- Publication Type:Journal Article
- MeSH:
Cell Proliferation;
drug effects;
Down-Regulation;
Humans;
K562 Cells;
Nuclear Proteins;
metabolism;
Phosphoprotein Phosphatases;
metabolism;
Tyrphostins;
pharmacology
- From:
Journal of Experimental Hematology
2012;20(4):889-892
- CountryChina
- Language:Chinese
-
Abstract:
This study was aimed to investigate the effect of AG490, a JAK2 inhibitor, on expression of PHLPP and p-Akt in K562. K562 cells were treated with different concentrations of AG490. The proliferation of K562 cells was examined by WST-1 assay and apoptosis of K562 cells was detected by flow cytometry with Annexin V-FITC/PI double staining. The expressions of PHLPP, phosphorate-Akt (p-Akt) and total Akt protein were detected by Western blot. The results indicated that AG490 inhibited the proliferation of K562 cells in concentration-and time-dependent manners, with the IC(50) 338.0 µmol/L in 48 h. AG490 100 µmol/L also induced apoptosis of K562 cells in a time-dependent manner. AG490 100 µmol/L time-dependently down-regulated the protein expression of p-Akt and PHLPP, but without significant effect on expression of total Akt. It is concluded that AG490 can inhibit proliferation and induce apoptosis of K562 cells through down-regulation of p-Akt expression, but inhibiting efficacy of AG490 on K562 proliferation also may be limited due to the down-regulation of p-Akt regulatory protein PHLPP expression.
