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Submit ReviewCGP 57380
Description: Selective inhibitor of Mnk1
Chemical Name: N3-(4-Fluorophenyl)-1H-pyrazolo-[3,4-d]pyrimidine-3,4-diamine
Purity: ≥98% (HPLC)
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
CGP 57380 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for CGP 57380
| M. Wt | 244.23 |
| Formula | C11H9FN6 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 522629-08-9 |
| PubChem ID | 11644425 |
| InChI Key | UQPMANVRZYYQMD-UHFFFAOYSA-N |
| Smiles | NC1=C2C(NC3=CC=C(F)C=C3)=NNC2=NC=N1 |
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 | |
|---|---|---|---|
| Solubility | |||
| DMSO | 24.42 | 100 |
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 |
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Product Datasheets for CGP 57380
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
If you know of a relevant reference for CGP 57380, please let us know.
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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:
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
Brown and Gromeier (2017) MNK Controls mTORC1:Substrate Association through Regulation of TELO2 Binding with mTORC1. Cell Rep 18 1444 PMID: 28178522
Origanti et al (2012) Ornithine decarboxylase mRNA is stabilized in an mTORC1-dependent manner in Ras-transformed cells. Biochem J 442 199 PMID: 22070140
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
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
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
Do you know of a great paper that uses CGP 57380 from Tocris? Please let us know.
Reviews for CGP 57380
Average Rating: 3 (Based on 1 Review.)
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(CGP57380, 10 μM).
By
Anonymous on 12/11/2019
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: LP-1 cell line
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
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.