Cat. No.: HY-182914

NGI-189

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Based on 1 Customer Validation

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.

For research use only. We do not sell to patients.

Purity: 99.29%
CAS No.: 2763063-26-7
Formula: C₂₂H₃₀N₄O₄S₂
Molecular Weight:478.63

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

NGI-189 Chemical Structure

CAS No.: 2763063-26-7

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

Akt

EGFR^L858R/T790M

EGFR

Bim

All EGFR Isoforms :

All Akt Isoforms :

All Bcl-2 Family Isoforms :

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.

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 mm³by 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 mm³by 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.

Chemical Information

CAS No. 2763063-26-7
Appearance Solid
Molecular Weight 478.63
Formula C₂₂H₃₀N₄O₄S₂
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0893 mL

10.4465 mL

20.8930 mL

5 mM

0.4179 mL

2.0893 mL

4.1786 mL

10 mM

0.2089 mL

1.0446 mL

2.0893 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Baro M, et al. Redundancy of the OST catalytic subunit facilitates therapeutic targeting of N-glycosylation. Cell Chem Biol. 2025;32(6):839-853.e6. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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NGI-189

Apoptosis Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Glutamine Metabolism Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Mitochondria-Targeted Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

All EGFR Isoforms

All Akt Isoforms

All Bcl-2 Family Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

NGI-189 Related Classifications

Cat. No.: HY-182914