CGP 57380

Cat. No. 2731

CGP 57380 C11H9FN6 [522629-08-9]

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Chemical Name: N3-(4-Fluorophenyl)-1H-pyrazolo-[3,4-d]pyrimidine-3,4-diamine

Biological Activity

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

M.Wt:
244.23
Formula:
C11H9FN6
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
522629-08-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Andersson and Sundler (2006) Posttranscriptional regulation of TNFα expression via eukaryotic initiation factor 4E (eIF4E) phosphorylation in mouse macrophages. Cytokine 33 52. PMID: 16431125.

Ishida et al (2003) Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells. Circ.Res. 93 1218. PMID: 14605021.

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.

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Citations are publications that use Tocris products. Selected citations for CGP 57380 include:

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.

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.

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.

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Keywords: CGP 57380, supplier, Selective, inhibitors, inhibits, Mnk1, Kinases, CGP57380, Tocris Bioscience, Mnk Inhibitor products

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