EB1 is the inhibitor of kinases MNK with IC50s of 0.69 μM (MNK1) and 9.4 μM (MNK2). EB1 selectively inhibits the growth of cancer cells, but not normal cells. EB1 also increases cell apoptosis and suppresses eIF4E phosphorylation.
EB1 (1.3-40 μM; 24 hr) inhibits the phosphorylation of eIF4E dose-dependently[1].EB1 (2.5-40 μM; 72 hr) shows dose-dependent cytotoxicity on tumor cells, and induces apoptosis[1].EB1 (5 μM, 10 μM, and 20 μM; 24 hr) acts directly on MNK kinases without perturbing activating upstream signaling, such as activation of p38 (p-p38) and phosphorylation of its downstream effector HSP27[1].EB1 (compound 14) inhibits the growth of HepG2 and MCF-7 cancer cells with IC50s of 0.74 μM and 5.18 μM, respectively[2].
References:
[1]. Bou-Petit E, et al. Overcoming Paradoxical Kinase Priming by a Novel MNK1 Inhibitor. J Med Chem. 2022 Apr 28;65(8):6070-6087.
[2]. Aboukhatwa SM, et al. Nicotinonitrile-derived apoptotic inducers: Design, synthesis, X-ray crystal structure and Pim kinase inhibition. Bioorg Chem. 2022 Dec;129:106126.