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NFPA 704
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2
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CGP 57380 C화학적 특성, 용도, 생산
용도
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
생물학적 활성
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).
