Biological Activity
Inhibitor of MAP-kinase interacting kinase-1 (Mnk1, MKNK1) (IC 50 = 2.2 μ M) that displays selectivity over p38, JNK1, ERK1, ERK2, PKC and c-src family kinases. Blocks phosphorylation of eIF4E in cellular assays (IC 50 = 3 μ M) and inhibits LPS-induced TNF α expression in macrophages.
Biochem/physiol Actions
CGP 57380 is a β-catenin nuclear translocation inhibitor, which prevents the proliferation of several?cancers. It enhances radiation-induced apoptosis in nasopharyngeal carcinoma (NPC). CGP 57380 upregulates β-catenin in the cytoplasm and inhibits epithelial-mesenchymal transition (EMT).
References
[1]. knauf u, tschopp c, gram h. negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. mol cell biol, 2001, 21(16): 5500-5511.
[2]. ishida m, ishida t, nakashima h, et al. mnk1 is required for angiotensin ii-induced protein synthesis in vascular smooth muscle cells. circ res, 2003, 93(12): 1218-1224.
[3]. andersson k, sundler r. posttranscriptional regulation of tnfalpha expression via eukaryotic initiation factor 4e (eif4e) phosphorylation in mouse macrophages. cytokine, 2006, 33(1): 52-57.
[4]. rowlett rm, chrestensen ca, nyce m, et al. mnk kinases regulate multiple tlr pathways and innate proinflammatory cytokines in macrophages. am j physiol gastrointest liver physiol, 2008, 294(2): g452-459.
