Other grades of this product :
| CGP 57380 Basic information |
| Product Name: | CGP 57380 | | Synonyms: | CGP 57380;CGP57380, N3-(4-fluorophenyl)-1h-pyrazolo[3,4-d]pyrimidine-3,4-diamine;MNK1 Inhibitor;N3-(4-Fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidine-3,4-diamine;CGP57380; CGP-57380;CS-1420;MNK1 Inhibitor - CAS 522629-08-9 - Calbiochem;P 57380 | | CAS: | 522629-08-9 | | MF: | C11H9FN6 | | MW: | 244.23 | | EINECS: | | Product Categories: | Inhibitors | | Mol File: | 522629-08-9.mol |
| CGP 57380 Chemical Properties |
| storage temp. | 2-8°C | | solubility | DMSO: soluble10mg/mL, clear | | form | powder | | color | white to beige |
| WGK Germany | 3 | | HS Code | 2933599590 |
| CGP 57380 Usage And Synthesis |
| 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
| | 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. |
| CGP 57380 Preparation Products And Raw materials |
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