CGP 57380

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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 (7)
Reviews (1)
Literature (3)

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 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. 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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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 the degree 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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References

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:

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

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


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Reviews for CGP 57380

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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).

PMID: 27626179
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