cgp-57380

Description: CGP 57380 is a potent, cell-permeable and selcetive MNK1 inhibitor with IC50 of 2.2 uM, it exhibited no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases. In 293 cells, CGP 57380 (10 uM) inhibited eIF4E phosphorylation in response to fetal calf serum (FCS), arsenite, anisomycin, PMA or tumor necrosis factor alpha. Also, CGP 57380 increased the cap-dependent reporter rluc. In cellular assays, CGP 57380 inhibited eIF4E phosphorylation with IC50 value of 3 uM. In rat vascular smooth muscle cells, CGP 57380 inhibited eIF4E phosphorylation, protein synthesis and VSMC hypertrophy induced by angiotensin II in a dose dependent way.

References: Mol Cell Biol. 2001; 21:5500-11; Circ Res. 2003; 93:1218-24; Proc Natl Acad Sci U S A. 2013; 110:E2298-307.