CGP 57380

Name: CGP 57380
Brand: Tocris Bioscience
SKU: 2731
Rating: 3 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 2731

(1)

Citations (40)

COA / SDS

Selective inhibitor of Mnk1

Key Product Details

Description:	Selective inhibitor of Mnk1
Chemical Name:	N³-(4-Fluorophenyl)-1H-pyrazolo-[3,4-d]pyrimidine-3,4-diamine
Purity:	≥98% (HPLC)
Molecular Weight:	244.23

View Full Technical Details for CGP 57380

Technical Data
Citations / Reviews (1)

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 for CGP 57380

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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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References for CGP 57380

References are publications that support the biological activity of the product.

Ishida Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells. Circ.Res. 2003 PMID: 14605021
Andersson and Sundler Posttranscriptional regulation of TNFα expression via eukaryotic initiation factor 4E (eIF4E) phosphorylation in mouse macrophages. Cytokine 2006 PMID: 16431125
Knauf Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. Mol.Cell.Biol. 2001 PMID: 11463832