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Biological Activity for CGP 57380
CGP 57380 is an inhibitor of MAP-kinase interacting kinase-1 (Mnk1, MKNK1) (IC50 = 2.2 μM) that displays selectivity over p38, JNK1, ERK1, ERK2, PKC and c-src family kinases. Blocks phosphorylation of eIF4E in cellular assays (IC50 = 3 μM) and inhibits LPS-induced TNFα expression in macrophages.
Compound Libraries for CGP 57380
Technical Data for CGP 57380
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CGP 57380
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for CGP 57380
The following data is based on the product molecular weight 244.23. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||4.09 mL||20.47 mL||40.95 mL|
|5 mM||0.82 mL||4.09 mL||8.19 mL|
|10 mM||0.41 mL||2.05 mL||4.09 mL|
|50 mM||0.08 mL||0.41 mL||0.82 mL|
References for CGP 57380
References are publications that support the biological activity of the product.
Knauf et al (2001) Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. Mol.Cell.Biol. 21 5500 PMID: 11463832
Ishida et al (2003) Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells. Circ.Res. 93 1218 PMID: 14605021
Andersson and Sundler (2006) Posttranscriptional regulation of TNFα expression via eukaryotic initiation factor 4E (eIF4E) phosphorylation in mouse macrophages. Cytokine 33 52 PMID: 16431125
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Keywords: CGP 57380, CGP 57380 supplier, Selective, inhibitors, inhibits, Mnk1, Kinases, CGP57380, Mnk, 2731, Tocris Bioscience
7 Citations for CGP 57380
Citations are publications that use Tocris products. Selected citations for CGP 57380 include:
Melemedjian et al (2010) IL-6- and NGF-induced rapid control of protein synthesis and nociceptive plasticity via convergent signaling to the eIF4F complex. J Neurosci 30 15113 PMID: 21068317
Riz et al (2016) Noncanonical SQSTM1/p62-Nrf2 pathway activation mediates proteasome inhibitor resistance in multiple myeloma cells via redox, metabolic and translational reprogramming. Oncotarget 7 66360 PMID: 27626179
Dumoulin et al (2013) Extracellular Signal-Regulated Kinase (ERK) Activity During Sleep Consolidates Cortical Plasticity In Vivo. Cereb Cortex PMID: 24047601
Origanti et al (2012) Ornithine decarboxylase mRNA is stabilized in an mTORC1-dependent manner in Ras-transformed cells. Biochem J 442 199 PMID: 22070140
Brown and Gromeier (2017) MNK Controls mTORC1:Substrate Association through Regulation of TELO2 Binding with mTORC1. Cell Rep 18 1444 PMID: 28178522
Brown et al (2014) Mitogen-activated protein kinase-interacting kinase regulates mTOR/AKT signaling and controls the serine/arginine-rich protein kinase-responsive type 1 internal ribosome entry site-mediated translation and viral oncolysis. J Biol Chem 88 13149 PMID: 25187540
Royall et al (2015) Murine norovirus 1 (MNV1) replication induces translational control of the host by regulating eIF4E activity during infection. Neurochem Res 290 4748 PMID: 25561727
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Reviews for CGP 57380
Average Rating: 3 (Based on 1 Review.)
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Cells were treated with MG-132 (15 µM) for 18 hours in the absence or presence of an eIF4E/eIF4G interaction inhibitor (4EGI-1, 50 µM) or an MNK inhibitor (CGP57380, 10 μM).
Literature in this Area
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MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.