A cell-permeable 3,5-disubstituted pyrazolo compound that acts as a selective MNK inhibitor (IC₅₀ = 646 and 575 nM, respectively, against MNK1 and MNK2) with much reduced or little activity against a panel of 24 other kinases (≤15% inhibition at 5 µM), including MNK upstream kinases B-Raf, ERK1, MEK1, and p38α. Reported to exhibit good aqueous solubility (>100 µM at pH 7.4) and inhibit the proliferation (IC₅₀ = 17 µM) and cellular eIF4E Ser²⁰⁹ phosphorylation (IC₅₀ = 4.7 µM) of acute myeloid leukemia MV4:11 cells.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Oyarzabal, J., et al. 2010. J. Med. Chem.53, 6618.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)