Chemical Name:N3-(4-Fluorophenyl)-1H-pyrazolo-[3,4-d]pyrimidine-3,4-d
iamine
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.
Knaufet al
(2001) Negative regulation of protein translation by mitogen-activated protein
kinase-interacting kinases 1 and 2. Mol.Cell.Biol. 21 5500. Ishidaet al (2003) Mnk1 is required for angiotensin II-induced protein
synthesis in vascular smooth muscle cells. Circ.Res. 93 1218. Andersson
and Sundler (2006) Posttranscriptional regulation of TNFα expression via eukaryotic
initiation factor 4E (eIF4E) phosphorylation in mouse macrophages. Cytokine 33
52.