NGI-1, also known as ML414, is a potent oligosaccharyltransferase (OST) inhibitor that directly targets and blocks the function of the OST catalytic subunits STT3A and STT3B[1].NGI-1 effectively reduces viral infectivity without affecting cell viability. NGI-1 blocks N-linked glycosylation of EGFR in lung adenocarcinoma cells and results in altered cellular localisation of the EGFR[2].
NGI-1 细胞实验
Cell Line
Concentration
Treated Time
Description
References
H1975-OR
10μM
5 days
NGI-1 reduced proliferation of H1975-OR cells by ~70% and caused G1 cell cycle arrest.
Cancer Res. 2018 Sep 1;78(17):5094-5106.
HCC827-GR
10μM
5 days
NGI-1 reduced proliferation of HCC827-GR cells by ~80% and caused G1 cell cycle arrest.
Cancer Res. 2018 Sep 1;78(17):5094-5106.
PC9-GR2
10μM
5 days
NGI-1 reduced proliferation of PC9-GR2 cells by ~90% and caused G1 cell cycle arrest.
Cancer Res. 2018 Sep 1;78(17):5094-5106.
Huh7 cells
8 μM
48 hours
NGI-1 significantly reduced DENV and ZIKV infectivity
Cell Rep. 2017 Dec 12;21(11):3032-3039.
PC9-GR1
10μM
5 days
NGI-1 reduced proliferation of PC9-GR1 cells by ~90% and caused G1 cell cycle arrest.
Cancer Res. 2018 Sep 1;78(17):5094-5106.
T98G
10 μM
48 hours
NGI-1 reduced phosphorylation of PDGFR but had no significant effect on radiosensitivity in T98G cells.
Clin Cancer Res. 2019 Jan 15;25(2):784-795.
U251
10 μM
48 hours
NGI-1 reduced phosphorylation of MET but had no significant effect on radiosensitivity in U251 cells.
Clin Cancer Res. 2019 Jan 15;25(2):784-795.
SKMG3
10 μM
48 hours
NGI-1 reduced protein levels of ErbB2 and ErbB3, and enhanced radiosensitivity in SKMG3 cells.
Clin Cancer Res. 2019 Jan 15;25(2):784-795.
D54
10 μM
48 hours
NGI-1 reduced glycosylation and phosphorylation of EGFR, ErbB2, and ErbB3, and enhanced radiosensitivity in D54 cells.
Clin Cancer Res. 2019 Jan 15;25(2):784-795.
HN4 cells
0-20 μmol/L
24 hours
Inhibited STT3B-mediated glycosylation of EREG, leading to its degradation and suppression of PDL1
Int J Oral Sci. 2024 Jul 1;16(1):47.
HEK293T-ACE2 cells
1 μM
48 hours
To evaluate the effect of NGI-1 on SARS-CoV-2 and its variant pseudovirus infectivity, results showed that NGI-1 significantly reduced pseudovirus infectivity.
EBioMedicine. 2021 Dec;74:103712.
Vero E6 cells
1.863 μM
1 hour pretreatment
To evaluate the effect of NGI-1 on SARS-CoV-2 infectivity, results showed that NGI-1 significantly reduced viral protein expression and infectivity.
EBioMedicine. 2021 Dec;74:103712.
HEK293T cells
10 μM
24 hours
To evaluate the effect of NGI-1 on SARS-CoV-2 spike protein glycosylation, results showed that NGI-1 treatment reduced the molecular weight of spike protein, indicating glycosylation inhibition.
EBioMedicine. 2021 Dec;74:103712.
HEK293 cells
1 μM and higher
48 hours
NGI-1 significantly inhibited DENV and ZIKV replication with EC50 values of 0.85 μM and 2.2 μM, respectively
Cell Rep. 2017 Dec 12;21(11):3032-3039.
Madin-Darby canine kidney (MDCK) epithelial cells
10.0 μM
1 hour to 24 hours
To evaluate the effect of NGI-1 on influenza virus growth, results showed that NGI-1 treatment significantly reduced the infectious titers of influenza viruses
mBio. 2022 Apr 26;13(2):e0298321.
Normal human bronchial epithelial (NHBE) cells
10.0 μM
1 hour to 24 hours
To evaluate the effect of NGI-1 on influenza virus growth, results showed that NGI-1 treatment significantly reduced the infectious titers of all tested influenza viruses
mBio. 2022 Apr 26;13(2):e0298321.
MCF7 breast carcinoma cells
10 µM
48 hours
To evaluate the inhibitory effect of NGI-1 on protein glycosylation and its impact on entosis. Results showed that NGI-1 significantly increased the number of entotic structures and increased the proportion of apoptotic+necrotic cells after ROCKi treatment.
Cell Death Dis. 2022 Aug 24;13(8):730.
293T cells
10 μM
24 hours
Inhibited glycosylation of LAMP1 and LAMP2A, similar to the effects observed with ALKBH1 overexpression
Cell Mol Life Sci. 2024 Mar 12;81(1):130.
HeLa cells
10 μM
24 hours
Inhibited glycosylation of LAMP1 and LAMP2A, similar to the effects observed with ALKBH1 overexpression
Cell Mol Life Sci. 2024 Mar 12;81(1):130.
NGI-1 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Female athymic Swiss nu/nu mice
HCC827-GR and H1975-OR xenografts
Intravenous injection
20 mg/kg
Three times per week for a total of 8 doses
NGI-1 nanoparticles significantly delayed the growth of HCC827-GR and H1975-OR xenografts, with enhanced effects when combined with EGFR TKIs.
Cancer Res. 2018 Sep 1;78(17):5094-5106.
Nude mice
D54 and SKMG3 xenograft models
Intravenous injection
20 mg/kg
Every other day for a total of 3 doses
NGI-1 NPs significantly inhibited the growth of D54 and SKMG3 xenografts and showed better efficacy when combined with radiotherapy.
Clin Cancer Res. 2019 Jan 15;25(2):784-795.
C57BL/6 mice
MTCQ1 syngeneic model
Intraperitoneal injection
10 mg/kg
4 times per week, during treatment
Combination of NGI-1 with anti-PDL1 therapy significantly enhanced immunotherapy efficacy
Int J Oral Sci. 2024 Jul 1;16(1):47.
BALB/c nude mice
Xenograft tumor model
Intraperitoneal injection
20 mg/kg
3 times per week for a total of 8 doses
NGI-1 significantly inhibited the growth of PC-9 xenograft tumors, reducing tumor volume and wet weight
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