| Identification | Back Directory | [Name]
CGP 57380 | [CAS]
522629-08-9 | [Synonyms]
CS-1420
P 57380
CGP 57380
MNK1 Inhibitor
CGP57380; CGP-57380
MNK1 Inhibitor - CAS 522629-08-9 - Calbiochem
N3-(4-Fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidine-3,4-diamine
1H-Pyrazolo[3,4-d]pyrimidine-3,4-diamine, N3-(4-fluorophenyl)-
CGP57380, N3-(4-fluorophenyl)-1h-pyrazolo[3,4-d]pyrimidine-3,4-diamine | [Molecular Formula]
C11H9FN6 | [MDL Number]
MFCD03861062 | [MOL File]
522629-08-9.mol | [Molecular Weight]
244.23 |
| Hazard Information | Back Directory | [Uses]
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
| [Definition]
ChEBI: N3-(4-fluorophenyl)-2H-pyrazolo[3,4-d]pyrimidine-3,4-diamine is a pyrazolopyrimidine. | [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). | [storage]
Store at +4°C | [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. |
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