An OST inhibitor
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NGI 1 is an oligosaccharyltransferase (OST) inhibitor.1 It binds to and stabilizes the STT3B catalytic subunit of OST in a cellular thermal shift assay (CETSA) and inhibits N-linked glycosylation in a reporter assay using D54 ER-LucT cells (IC50 = 1.1 ?M). NGI 1 (10 ?M) reduces glycosylation and membrane localization of EGFR in H3255 lung adenocarcinoma cells and inhibits proliferation of PC-9 and A549 non-small cell lung cancer (NSCLC) cells. It inhibits dengue and Zika virus replication in HEK293 cells (EC50s = 0.85 and 2.2 ?M, respectively).2 NGI 1 also reduces viral RNA in HEK293 cells infected with West Nile virus or yellow fever virus.
1.Lopez-Sambrooks, C., Shrimal, S., Khodier, C., et al.Oligosaccharyltransferase inhibition induces senescence in RTK-driven tumor cellsNat. Chem. Biol.12(12)1023-1030(2016) 2.Puschnik, A.S., Marceau, C.D., Ooi, Y.S., et al.A small-molecule oligosaccharyltransferase inhibitor with pan-flaviviral activityCell Rep.21(11)3032-3039(2017)
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