CGP 57380
Chemical Name: N3-(4-Fluorophenyl)-1H-pyrazolo-[3,4-d]pyrimidine-3,4-diamine
Purity: ≥98%
Biological Activity
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.Technical Data
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.
Background References
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Murine norovirus 1 (MNV1) replication induces translational control of the host by regulating eIF4E activity during infection.
Royall E, Doyle N, Abdul-Wahab A, Emmott E, Morley S, Goodfellow I, Roberts L, Locker N
J Biol Chem, 2015;290(8):4748-58. -
Cotargeting MNK and MEK kinases induces the regression of NF1-mutant cancers
J Clin Invest, 2016;0(0):. -
MNK Controls mTORC1:Substrate Association through Regulation of TELO2 Binding with mTORC1
MC Brown, M Gromeier
Cell Rep, 2017;18(6):1444-1457. -
Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2.
Knauf et al.
Mol.Cell.Biol., 2001;21:5500 -
Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells.
Ishida et al.
Circ.Res., 2003;93:1218 -
Posttranscriptional regulation of TNFα expression via eukaryotic initiation factor 4E (eIF4E) phosphorylation in mouse macrophages.
Andersson and Sundler
Cytokine, 2006;33:52
Product Datasheets
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Citations for CGP 57380
The citations listed below are publications that use Tocris products. Selected citations for CGP 57380 include:
7 Citations: Showing 1 - 7
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MNK Controls mTORC1:Substrate Association through Regulation of TELO2 Binding with mTORC1.
Authors: Brown and Gromeier
Cell Rep 2017;18:1444
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Noncanonical SQSTM1/p62-Nrf2 pathway activation mediates proteasome inhibitor resistance in multiple myeloma cells via redox, metabolic and translational reprogramming.
Authors: Riz Et al.
Oncotarget 2016;7:66360
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Murine norovirus 1 (MNV1) replication induces translational control of the host by regulating eIF4E activity during infection.
Authors: Royall Et al.
Neurochem Res 2015;290:4748
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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.
Authors: Brown Et al.
J Biol Chem 2014;88:13149
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Extracellular Signal-Regulated Kinase (ERK) Activity During Sleep Consolidates Cortical Plasticity In Vivo.
Authors: Dumoulin Et al.
Cereb Cortex 2013;
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Ornithine decarboxylase mRNA is stabilized in an mTORC1-dependent manner in Ras-transformed cells.
Authors: Origanti Et al.
Biochem J 2012;442:199
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IL-6- and NGF-induced rapid control of protein synthesis and nociceptive plasticity via convergent signaling to the eIF4F complex.
Authors: Melemedjian Et al.
J Neurosci 2010;30:15113
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