NSP-1047 is a potent, selective inhibitor of MAPK-interacting kinases MNK1 and MNK2 with IC50 of 0.5 nM and 0.1 nM respectively.
NSP-1047 demonstrates remarkable in vitro inhibition of eIF4E phosphorylation with IC50 of 0.2 nM in OCI-Ly7 cells.
NSP-1047 binds to the ATP active site of MNK2.
NSP-1047 exhibits good kinase selectivity against a panel of 211 kinases at 0.5 uM.
NSP-1047 effectively inhibits the expression of various immune checkpoint proteins in vitro, including PD-1, LAG-3, TIM-3, CTLA-4 and VISITA, while also reducing the expression of pro-inflammatory cytokines such as IFN-γ, IL-8 and TNF-α.
NSP-1047 displays inhibitory effects across 14 AML tumor cell lines with IC50 values of <1 uM in MV-4-11, Molm-13, KASUMI-1, and OCI-AML-1 cell lines.
NSP-1047 exhibits significant antitumor activity in animal models, particularly in combination with low doses of Ara-C (cytarabine) or with venetoclax.