2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Apoptosis
  3. EGFR Akt Bcl-2 Family Apoptosis
  4. NGI-189

NGI‑189 is a selective OST‑A inhibitor. NGI‑189 inhibits the STT3A catalytic subunit of the OST complex and reduces N‑glycosylation of target glycoproteins. NGI‑189 blocks oncogenic and bypass signaling, reduces phosphorylation of EGFR, AKT, p70S6K and S6RP, and induces cell cycle arrest and apoptosis. NGI‑189 markedly suppresses tumor growth and induces tumor regression in non‑small cell lung cancer (NSCLC) xenograft models. NGI‑189 can be used for the research of EGFR‑mutant non‑small cell lung cancer.

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NGI-189

NGI-189 Chemical Structure

CAS No. : 2763063-26-7

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10 mM * 1 mL in DMSO
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NGI-189 Related Antibodies

Top Publications Citing Use of Products

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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Akt Akt1 Akt2 Akt3

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • Biological Activity

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Description

NGI‑189 is a selective OST‑A inhibitor. NGI‑189 inhibits the STT3A catalytic subunit of the OST complex and reduces N‑glycosylation of target glycoproteins. NGI‑189 blocks oncogenic and bypass signaling, reduces phosphorylation of EGFR, AKT, p70S6K and S6RP, and induces cell cycle arrest and apoptosis. NGI‑189 markedly suppresses tumor growth and induces tumor regression in non‑small cell lung cancer (NSCLC) xenograft models. NGI‑189 can be used for the research of EGFR‑mutant non‑small cell lung cancer[1].

IC50 & Target[1]

Akt

 

EGFRL858R/T790M

 

EGFR

 

Bim

 

In Vitro

NGI-189 (0.09 μM) potently inhibits N-glycosylation in ER-LucT reporter cells with an IC50 of 0.09 μM[1].
NGI-189 (5 μM; 5 days) inhibits proliferation of parental PC9 EGFR mutant NSCLC cells by ~70%, with significant rescue observed in PC9-CD8-EGFR-CL cells that express N-glycosylation-independent EGFR[1].
NGI-189 (0-25 μM; 24 h) preferentially inhibits the OST-A complex in HEK293 wild-type, STT3A KO, and STT3B KO cells, reducing N-glycosylation of EGFR and Halo3N in a dose-dependent manner, with complete inhibition of OST-A-dependent glycosylation achievable only in STT3B KO cells[1].
NGI-189 (10 μM; 24 h) reduces N-glycosylation of bypass PTK7, MET and inhibits downstream STAT3 signaling in Osimertinib (HY-15772)-resistant H1975-OR and Gefitinib (HY-50895)-resistant HCC827-GR NSCLC cells[1].
NGI‑189 (5 μM) reduces clonogenic survival of parental PC9 EGFR‑mutant NSCLC cells and shows significant rescue in PC9‑CD8‑EGFR‑CL cells expressing N‑glycosylation‑independent EGFR; it also significantly decreases clonogenic survival of H3255, HCC‑4006, and HCC‑2935 EGFR‑mutant NSCLC cells[1].
NGI-189 (5 μM; 24 h) inhibits EGFR and downstream AKT/p70S6K/S6RP signaling, and induces pro-apoptotic Bim protein expression in H3255, HCC-4006, and HCC-2935 EGFR mutant NSCLC cells[1].
NGI-189 (5 μM; 24 h) induces G1 phase cell cycle arrest in PC9 EGFR-mutant NSCLC cells, and triggers G1 arrest accompanied by marked cell death (sub-G1 population) in H3255 and HCC-2935 EGFR-mutant NSCLC cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NGI-189 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293 wild-type, STT3A knockout (KO), and STT3B KO cells expressing Halo3N glycoprotein
Concentration: 0 μM, 0.1 μM, 1 μM, 5 μM, 10 μM, 25 μM
Incubation Time: 24 h
Result: Reduced the molecular weight of EGFR and Halo3N in wild-type HEK293 cells at all tested concentrations, indicating reduced N-glycosylation.
Showed weaker inhibition of N-glycosylation in STT3A KO cells, while showed potent inhibition in STT3B KO cells, demonstrating preferential activity against the OST-A (STT3A-containing) complex.
Achieved complete inhibition of OST-A dependent N-glycosylation in STT3B KO cells at doses >10 μM, but could not achieve complete N-glycosylation inhibition in wild-type cells due to OST catalytic subunit redundancy.

Cell Proliferation Assay[1]

Cell Line: Parental PC9 EGFR mutant non-small cell lung cancer (NSCLC) cells, PC9-CD8-EGFR-CL (N-glycosylation-independent EGFR) cells
Concentration: 5 μM
Incubation Time: 5 days
Result: Reduced proliferation of parental PC9 cells by approximately 70%.
Showed significantly rescued proliferation of PC9-CD8-EGFR-CL cells relative to parental cells, confirming the anti-proliferative effect is mediated via inhibition of EGFR N-glycosylation.

Western Blot Analysis[1]

Cell Line: PC9 EGFR mutant NSCLC cells
Concentration: 1 μM, 5 μM
Incubation Time: 24 h
Result: Caused dose-dependent inhibition of EGFR Y1068 phosphorylation, accompanied by reduced phosphorylation of AKT S473, p70 S6K T389, and S6RP S235-236.
Induced increased levels of the pro-apoptotic protein Bim at both tested concentrations.

Cell Cycle Analysis[1]

Cell Line: PC9 EGFR mutant NSCLC cells
Concentration: 5 μM
Incubation Time: 24 h
Result: Induced a greater accumulation of PC9 cells in the G1 phase of the cell cycle compared to vehicle control, indicating G1 cell cycle arrest.

Western Blot Analysis[1]

Cell Line: H3255 (EGFR L858R), HCC-4006 (EGFR del747-749, A750P), and HCC-2935 (EGFR del746-751, S752I) EGFR mutant NSCLC cells
Concentration: 5 μM
Incubation Time: 24 h
Result: Inhibited EGFR Y1068 phosphorylation, reduced phosphorylation of AKT S473, p70 S6K T389, and S6RP S235-236, and induced increased levels of Bim in all three EGFR mutant NSCLC cell lines.

Cell Cycle Analysis[1]

Cell Line: H3255 and HCC-2935 EGFR mutant NSCLC cells
Concentration: 5 μM
Incubation Time: 24 h
Result: Induced a modest increase in G1 cell cycle arrest and a significant increase in the sub-G1 populationl, indicating induction of cell death.

Western Blot Analysis[1]

Cell Line: H1975-OR (osimertinib-resistant, EGFR L858R/T790M) and HCC827-GR (gefitinib-resistant, EGFR del19/MET-amplified) NSCLC cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Reduced PTK7 N-glycosylation and inhibited STAT3 Y705 phosphorylation in H1975-OR cells.
Reduced PTK7 and MET N-glycosylation and inhibited STAT3 Y705 phosphorylation in HCC827-GR cells.
In Vivo

NGI-189 (10 mg/kg; i.p.; every other day; 8 total doses) elicits significant tumor growth delay in EGFR-mutant NSCLC PDX models as well as in gefitinib-resistant HCC827-GR NSCLC xenograft models[1].
NGI-189 (10 mg/kg; i.p.; every other day) induces significant tumor regression in osimertinib-resistant H1975-OR NSCLC xenografts[1].
NGI-189 (10 mg/kg; i.p.; every other day; 3 total doses) is well tolerated in mice, with no significant toxicity detected in blood work or organ histopathology[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NSG mice (female, 6-8 weeks old, immunodeficient)[1]
Dosage: 10 mg/kg
Administration: i.p.; every other day; 8 total doses
Result: Kept tumor volume at 193 mm3 by Day 8, while vehicle-treated tumors grew to 450 mm3.
Doubled the time for tumors to reach 500 mm3.
Reduced EGFR protein levels in tumors.
Showed weight changes similar to vehicle-treated mice.\nKept tumor volume at 167 mm3 by Day 12, while vehicle-treated tumors grew to 414 mm3.
Doubled the time for tumors to reach 500 mm3.
Showed significantly higher body weight at the end of treatment compared to vehicle controls.
Animal Model: athymic Swiss nu/nu mice (female, 6-8 weeks old)[1]
Dosage: 10 mg/kg
Administration: i.p.; every other day
Result: Induced significant tumor regression.
Achieved 60% of treated mice remaining progression-free at Day 90, compared to 0% of vehicle-treated mice.
Showed weight changes similar to vehicle-treated mice.
Animal Model: athymic Swiss nu/nu mice (female, 6-8 weeks old)[1]
Dosage: 10 mg/kg
Administration: i.p.; every other day; 8 total doses
Result: Limited tumor volume to 400 mm3 by Day 20.
Prolonged the time for tumors to reach 500 mm3.
Showed weight changes similar to vehicle-treated mice.
Animal Model: athymic Swiss nu/nu mice (female, 6-8 weeks old)[1]
Dosage: 10 mg/kg
Administration: i.p.; every other day; 3 total doses
Result: Showed no significant differences from vehicle-treated mice in blood counts, serum chemistries, or organ cytopathology.
Had only minor age-related abnormalities, same as vehicle group.
Molecular Weight

478.63

Formula

C22H30N4O4S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC(S(=O)(N2CCOCC2)=O)=CC=C1N(C3CCCC3)C)NC4=NC=C(CC)S4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (208.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0893 mL 10.4465 mL 20.8930 mL
5 mM 0.4179 mL 2.0893 mL 4.1786 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0893 mL 10.4465 mL 20.8930 mL 52.2324 mL
5 mM 0.4179 mL 2.0893 mL 4.1786 mL 10.4465 mL
10 mM 0.2089 mL 1.0446 mL 2.0893 mL 5.2232 mL
15 mM 0.1393 mL 0.6964 mL 1.3929 mL 3.4822 mL
20 mM 0.1045 mL 0.5223 mL 1.0446 mL 2.6116 mL
25 mM 0.0836 mL 0.4179 mL 0.8357 mL 2.0893 mL
30 mM 0.0696 mL 0.3482 mL 0.6964 mL 1.7411 mL
40 mM 0.0522 mL 0.2612 mL 0.5223 mL 1.3058 mL
50 mM 0.0418 mL 0.2089 mL 0.4179 mL 1.0446 mL
60 mM 0.0348 mL 0.1741 mL 0.3482 mL 0.8705 mL
80 mM 0.0261 mL 0.1306 mL 0.2612 mL 0.6529 mL
100 mM 0.0209 mL 0.1045 mL 0.2089 mL 0.5223 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NGI-1892763063-26-7NGI189NGI 189EGFRAktBcl-2 FamilyApoptosisEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BMETp70 S6KSTT3A-containing oligosaccharyltransferase complexnon-small cell lung cancerSTT3AAKTS6RPN-glycosylationPTK7Inhibitorinhibitorinhibit

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