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.
| 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
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
Keywords: CGP 57380, supplier, Selective, inhibitors, inhibits, Mnk1, Kinases, CGP57380, Mnk, Mnk, Tocris Bioscience
