Art. -Nr.: HY-U00459

GSK2850163

(Synonyms: GSK163)

7 Cited Publications

Kundenbewertung

Based on 7 publication(s) in Google Scholar

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC₅₀s of 20 and 200 nM, respectively.

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Reinheit: 98.52%
CAS. Nr.: 2121989-91-9
Formel: C₂₄H₂₉Cl₂N₃O
Molecular Weight:446.41

Speicherung:

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

GSK2850163 Chemical Structure

CAS. Nr.: 2121989-91-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 20 nM (IRE1α kinase activity), 200 nM (IRE1α RNase activity)^[1]

In Vitro

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC₅₀s of 20 and 200 nM, respectively. The increased autophosphorylation of IRE1α could be reduced in a dose-dependent manner by GSK2850163. Increasing concentrations of GSK2850163 are capable of reducing the increased XBP 1 transcriptional activity. Two additional kinases are weakly inhibited by GSK2850163: Ron (IC₅₀=4.4 μM) and FGFR1 V561M (IC₅₀=17 μM)^[1].

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

Chemical Information

CAS. Nr. 2121989-91-9
Appearance Oil
Molecular Weight 446.41
Formel C₂₄H₂₉Cl₂N₃O
Color Colorless to yellow
SMILES

O=C(N(CCC1)C[C@]21CCN(CC3=CC=C(Cl)C(Cl)=C3)C2)NCC4=CC=C(C)C=C4
Synonyms

GSK163
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (7)

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Journal Impact Factor

Sci Signal

PERK inhibition attenuates vascular remodeling in pulmonary arterial hypertension caused by BMPR2 mutation. [Abstract]

2021 Jan 26;14(667):eabb3616. PMID: 33500333
Mucosal Immunol

Deficiency of immunoglobulin IgSF6 enhances antibacterial effects by promoting ER stress and the inflammatory response in intestinal macrophages. [Abstract]

2024 Apr;17(2):288-302. PMID: 38387824
Microb Pathog

BvrR of Brucella initiates microglial inflammation through the activation of the IRE1 pathway. [Abstract]

2026 Jan 21:108313. PMID: 41577152
Microbiologyopen

BvrR From Brucella abortus Induces Neuroinflammation Through IRE1-Mediated Activation of ATF2 and NF-κB. [Abstract]

2026 Feb;15(1):e70219. PMID: 41566528

GSK2850163 purchased from MedChemExpress. Usage Cited in: Microbiologyopen. 2026 Feb;15(1):e70219. [Abstract]

Western blot analysis of p‐IRE1, p‐ATF2, p‐p65, IL‐6, and TNF‐α protein levels treated with GSK2850163 (8 μM).

GSK2850163 purchased from MedChemExpress. Usage Cited in: Microbiologyopen. 2026 Feb;15(1):e70219. [Abstract]

ELISA measurement of IL‐6 and TNF‐α in supernatants treated with GSK2850163 (8 μM).

GSK2850163 purchased from MedChemExpress. Usage Cited in: Microbiologyopen. 2026 Feb;15(1):e70219. [Abstract]

RT‐qPCR analysis of IL6 and TNF‐α mRNA expression treated with GSK2850163 (8 μM).
Vet Microbiol

The PERK-eIF2α branch activates the NLRP3 inflammasome through the NF-κB signaling pathway to suppress NDV replication. [Abstract]

2026 May:316:110968. PMID: 41793984
Vet Microbiol

A rough Brucella mutant induced macrophage death depends on secretion activity of T4SS, but not on cellular Txnip- and Caspase-2-mediated signaling pathway. [Abstract]

2020 May;244:108648. PMID: 32402333
Res Sq

2025 May 22.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 67.5 mg/mL (151.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 50 mg/mL (112.00 mM; Need ultrasonic)

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

2.2401 mL

11.2005 mL

22.4009 mL

5 mM

0.4480 mL

2.2401 mL

4.4802 mL

10 mM

0.2240 mL

1.1200 mL

2.2401 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 2.25 mg/mL (5.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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: ≥ 2.25 mg/mL (5.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 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 (22.5 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

Protokoll

Cell Assay^[1]

PANC-1 cells are seeded into six-well plates at a density of 5.0×10³ cells/well in RPMI 1640 media containing 10% FBS. Cells are cotransfected with a pGL3-5x unfolded protein response element (UPRE)-luciferase reporter containing five repetitions of the XBP-1 DNA binding site and pRL-SV40 using the FuGENE6 transfection reagent. Forty-eight hours later, cells are treated with 2.5 mg/mL tunicamycin for 1 hour, followed by GSK2850163 treatment for 16 hours. Luciferase expression is measured using Dual-Glo Luciferase Assay kit and normalized to Renilla expression levels^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)

Verweise

[1]. Nestor O. Concha, et al. Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity. Molecular Pharmacology December 2015, 88 (6) 1011-1023.

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
Ethanol / DMSO	1 mM	2.2401 mL	11.2005 mL	22.4009 mL	56.0023 mL
	5 mM	0.4480 mL	2.2401 mL	4.4802 mL	11.2005 mL
	10 mM	0.2240 mL	1.1200 mL	2.2401 mL	5.6002 mL
	15 mM	0.1493 mL	0.7467 mL	1.4934 mL	3.7335 mL
	20 mM	0.1120 mL	0.5600 mL	1.1200 mL	2.8001 mL
	25 mM	0.0896 mL	0.4480 mL	0.8960 mL	2.2401 mL
	30 mM	0.0747 mL	0.3733 mL	0.7467 mL	1.8667 mL
	40 mM	0.0560 mL	0.2800 mL	0.5600 mL	1.4001 mL
	50 mM	0.0448 mL	0.2240 mL	0.4480 mL	1.1200 mL
	60 mM	0.0373 mL	0.1867 mL	0.3733 mL	0.9334 mL
	80 mM	0.0280 mL	0.1400 mL	0.2800 mL	0.7000 mL
	100 mM	0.0224 mL	0.1120 mL	0.2240 mL	0.5600 mL

Keywords

GSK2850163

7 Cited Publications

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GSK2850163

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Endoplasmic Reticulum Stress Compound Library

Targeted Diversity Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) GSK2850163

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK2850163

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Endoplasmic Reticulum Stress Compound Library

Targeted Diversity Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) GSK2850163

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK2850163 Related Classifications

HY-U00459 Related Classifications