Biochem/physiol Actions

Reversible: yes

Cell permeable: yes

Primary TargetMNK

General description

A cell-permeable thieno[2,3-d]pyrimidine compound that acts as a selective inhibitor of MAP kinase-interacting kinases 1 and 2 (Mnk1 and 2: IC₅₀ = 23 and 16 nM for MNK1 and MNK2, respectively). Displays much reduced activity against several other protein kinases and does not affect the phosphorylation of ERK, Akt, mTORC1, and ribosomal S6 kinase. Shown to strongly inhibit eIF4E phosphorylation (~1 µM) and abolished the activity completely at higher concentration in MDA-MB-231 and SSC25 cancer cell (~ 1 µM). Shown to be much more effective Mnk inhibitor than CGP57380 (Cat. No. 454861). Reported to inhibit the migration of mouse embryonic fibroblasts and MDA-MB-231 and SCC25 cells, but does not affect their viability and proliferation.

Legal Information

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

Other Notes

Beggs, J.E., et al. 2015. Biochem. J.467, 63.

Packaging

Packaged under inert gas

Reconstitution

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

Warning

Toxicity: Standard Handling (A)