NGI-1 (Synonyms: N-linked Glycosylation Inhibitor 1; ML414) |
Catalog No.GC33055
One-Click Copy Product Info
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NGI-1 (ML414) is an effective oligosaccharyl transferase (OST) inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 790702-57-7
Sample solution is provided at 25 µL, 10mM.
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NGI-1 (ML414) is an effective oligosaccharyl transferase (OST) inhibitor [1]. NGI-1 selectively inhibits the STT3A and STT3B subunits in the oligosaccharyl transferase (OST) complex, thereby blocking the N-linked glycosylation process of proteins [2-3]. NGI-1 is often used to study the regulation of glycosylation-dependent proteins such as EGFR in tumor cells and has certain anti-tumor potential [4].
In PC9 cells, NGI-1 (10μM; 48h) reduced the proliferation of both parental and T790M-expressing PC9 cell lines by approximately 90% [5]. In HEK293 cells, NGI-1 (5μM; 60min) treatment results in cell type-dependent dysfunction of HSV-1 [2]. In Caco2 cells, NGI-1 (1μM, 5μM; 3d) has a significant inhibitory effect on SARS-CoV-2 [6]. In SKMG3 cells, NGI-1 (10μM; 48h) disrupts RTK signaling in glioblastoma cells [7].
In oral squamous cell carcinoma xenograft model, combined inhibition of EREG glycosylation by targeting NGI-1 (10mg/kg; ip; 14d) significantly enhanced the efficacy of anti-PDL1 inhibitors in vivo [8]. In lung adenocarcinoma xenograft model, the tumor volume and wet weight of NGI-1 (20mg/kg; ip; 24d) treated mice were significantly smaller than those of the DMSO control group at the end point [9]. In CD24-WT nude mice, NGI-1 (20mg/kg; ip; 24d) treatment significantly inhibited tumor growth [10].
References:
[1]. Rinis N, Golden JE, Marceau CD, et al. Editing N-glycan site occupancy with small-molecule oligosaccharyltransferase inhibitors. Cell chemical biology. 2018 Oct 18; 25(10): 1231-1241.
[2]. Lu H, Cherepanova NA, Gilmore R, et al. Targeting STT3A-oligosaccharyltransferase with NGI-1 causes herpes simplex virus 1 dysfunction. The FASEB Journal. 2019 Feb 27;33(6):6801.
[3]. Harada Y, Ohkawa Y, Kizuka Y, et al. Oligosaccharyltransferase: a gatekeeper of health and tumor progression. International journal of molecular sciences. 2019 Dec 2; 20(23): 6074.
[4]. Cao Y, Yi W, Zhu Q. Glycosylation in the tumor immune response: the bitter side of sweetness: Glycosylation in the tumor immune response. Acta Biochimica et Biophysica Sinica. 2024 Jun 28; 56(8): 1184.
[5]. Lopez Sambrooks C, Baro M, Quijano A, et al. Oligosaccharyltransferase inhibition overcomes therapeutic resistance to EGFR tyrosine kinase inhibitors. Cancer research. 2018 Sep 1; 78(17): 5094-5106.
[6]. Huang YJ, Zhao H, Huang X, et al. Identification of oligosaccharyltransferase as a host target for inhibition of SARS-CoV-2 and its variants. Cell Discovery. 2021 Nov 30; 7(1): 116.
[7]. Baro M, Lopez Sambrooks C, Quijano A, et al. Oligosaccharyltransferase inhibition reduces receptor tyrosine kinase activation and enhances glioma radiosensitivity. Clinical Cancer Research. 2019 Jan 15; 25(2): 784-795.
[8]. Xu S, Wang H, Zhu Y, et al. Stabilization of EREG via STT3B-mediated N-glycosylation is critical for PDL1 upregulation and immune evasion in head and neck squamous cell carcinoma. International Journal of Oral Science. 2024 Jul 1; 16(1): 47.
[9]. Cheng J, Xia L, Hao X, et al, Tavolari S. Targeting STT3A produces an anti-tumor effect in lung adenocarcinoma by blocking the MAPK and PI3K/AKT signaling pathway. Translational Lung Cancer Research. 2022 Jun; 11(6): 1089.
[10]. Wang J, Zhang HM, Zhu GH, et al. STT3-mediated aberrant N-glycosylation of CD24 inhibits paclitaxel sensitivity in triple-negative breast cancer. Acta Pharmacologica Sinica. 2025 Apr; 46(4): 1097-1110.
| Cell experiment [1]: | |
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Cell lines |
PC9 cells |
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Preparation Method |
Growth rates were determined by CellTiter 96 NonRadioactive Cell Proliferation Assay (Promega) according to the manufacturer's directions. Briefly, NSCLC cells (2 × 103) untreated or treated with 10μM NGI-1, 100μM gefitinib, or 1μM osimertinib were seeded in triplicate in 96-wells plates and grown in culture medium containing 10% serum. The media were changed with or without new inhibitor every 48 hours. |
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Reaction Conditions |
10μM; 48h |
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Applications |
NGI-1 reduced the proliferation of both parental and T790M-expressing PC9 cell lines by approximately 90%. |
| Animal experiment [2]: | |
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Animal models |
Oral squamous cell carcinoma xenograft model |
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Preparation Method |
NGI-1 was diluted with 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline to a final concentration of 1mg/mL, and the PDL1 inhibitor was diluted with PBS to a final concentration of 0.5mg/mL. In animal experiments, SPF female C57BL/6 mice (6 weeks old) were used. MTCQ1 cells were used to establish a tumor xenograft model, and cells (5×106 cells/100μL PBS) were subcutaneously injected into the flank of mice, and tumor size was monitored 3 times a week. NGI-1 and PDL1 inhibitors were administered by abdominal injection 4 times a week at doses of 10mg/kg and 5mg/kg, respectively. |
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Dosage form |
10mg/kg; ip; 14d |
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Applications |
Combined inhibition of EREG glycosylation by targeting NGI-1 significantly enhanced the efficacy of anti-PDL1 inhibitors in vivo. |
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References: |
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| Cas No. | 790702-57-7 | SDF | |
| Synonyms | N-linked Glycosylation Inhibitor 1; ML414 | ||
| Canonical SMILES | O=C(NC1=NC=C(C)S1)C2=CC(S(=O)(N(C)C)=O)=CC=C2N3CCCC3 | ||
| Formula | C17H22N4O3S2 | M.Wt | 394.51 |
| Solubility | DMSO : 160 mg/mL (405.57 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5348 mL | 12.6739 mL | 25.3479 mL |
| 5 mM | 507 μL | 2.5348 mL | 5.0696 mL |
| 10 mM | 253.5 μL | 1.2674 mL | 2.5348 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)