CGP 57380

Pricing Availability Delivery Time Qty
Cat.No. 2731 - CGP 57380 | C11H9FN6 | CAS No. 522629-08-9
Description: Selective inhibitor of Mnk1
Chemical Name: N3-(4-Fluorophenyl)-1H-pyrazolo-[3,4-d]pyrimidine-3,4-diamine
Purity: ≥98% (HPLC)
Datasheet
Citations (3)
Literature

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.

Compound Libraries

CGP 57380 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 24.42 100

Preparing Stock Solutions

The following data is based on the product molecular weight 244.23. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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, supplier, Selective, inhibitors, inhibits, Mnk1, Kinases, CGP57380, Mnk, Tocris Bioscience

3 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

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


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Literature in this Area

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Cancer Research Product Guide

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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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MAPK Signaling

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.

Pathways for CGP 57380

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