NGI-189

NGI-189 is an oligosaccharyltransferase A (OST-A) complex inhibitor and a derivative of NGI 1 (Item No. 31519).¹ It inhibits the glycosylation of an endoplasmic reticulum reporter protein in cells (IC₅₀ = 90 nM) and selectively inhibits the glycosylation of EGFR in STT3A knockout HEK293 cells over STT3B knockout HEK293 cells, which lack expression of the OST-A and OST-B catalytic subunits, respectively. NGI-189 inhibits EGFR glycosylation in, and the survival of, NCI H3255, HCC4006, and HCC2935 non-small cell lung cancer (NSCLC) cells expressing EGFR^L858R, EGFR^{Δ747-749/A750P}, or EGFR^{Δ746-751/S752I}, respectively. It induces cell cycle arrest at the G₁ phase and reduces the proliferation of PC-9 NSCLC cells expressing the activating EGFR^Δ746-750 mutation. NGI-189 (10 mg/kg, i.p.) reduces tumor growth in patient-derived xenograft (PDX) mouse models of NSCLC containing EGFR-activating mutations.

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1. Baro, M., Lee, H., Kelley, V., et al. Redundancy of the OST catalytic subunit facilitates therapeutic targeting of N-glycosylation. Cell Chem. Biol. 32(6), 839-853.e836 (2025).