ЦГП 57380

Использование

CGP 57380 has been used:

• as a mitogen-activated protein kinase-interacting kinase 1 (MNK1) inhibitor to investigate the role of Mnk1 on eukaryotic translation initiation factor 4F (eIF4F) assembly and Newcastle disease virus (NDV) replication in HeLa cells
• as an MNK1 inhibitor to block eIF4 complex to evaluate the contribution of interferon (IFN-γ) translation during m157- transgenic (Tg) stimulation
• as a β-catenin nuclear translocation inhibitor to analyze its effects on cytoplasmic and nuclear fractions of cells

Биологическая активность

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.

Биохимия/физиол Действия

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).