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.

Product Specifications

Molecular Weight

244.23

Formula

C₁₁H₉FN₆

Storage

Store at +4°C

Purity

≥98% (HPLC)

Chemical Name

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

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.

Solubility

	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 all 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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Background References

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

CGP 57380

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

Key Product Details

Description

View all Mnk Inhibitors »

Product Description