A cell-permeable 3,5-disubstituted pyrazolo compound that acts as a selective MNK inhibitor (IC50=646 and 575nM, respectively, against MNK1 and MNK2) with much reduced or little activity against 24 other kinases (<15% inhibition at 5uM). Reported to exhibit good aqueous solubility (>100uM at pH 7.4) and inhibit the proliferation (IC50=17uM) and cellular eIF4E Ser209 phosphorylation (IC50=4.7uM) of MV4:11 cells.
Molecular Formula:C₁₃H₁₆N₄•2HCl
Solubility:H2O
Molecular Weight:301.2
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
