GSK2850163
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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- Pureza: 98.52%
- No. CAS: 2121989-91-9
- Fòrmula: C24H29Cl2N3O
- Peso molecular:446.41
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) GSK2850163
More- Sci Signal. 2021 Jan 26;14(667):eabb3616. [Abstract]
- Mucosal Immunol. 2024 Apr;17(2):288-302. [Abstract]
- Microb Pathog. 2026 Jan 21:108313. [Abstract]
- Microbiologyopen. 2026 Feb;15(1):e70219. [Abstract]
- Vet Microbiol. 2026 May:316:110968. [Abstract]
- Vet Microbiol. 2020 May;244:108648. [Abstract]
- Res Sq. 2025 May 22.
Customer Validation & Images
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ELISA
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Actividad biológica
IC50: 20 nM (IRE1α kinase activity), 200 nM (IRE1α RNase activity)[1]
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
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No. CAS 2121989-91-9
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Appearance Oil
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Peso molecular 446.41
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Fòrmula C24H29Cl2N3O
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Color Colorless to yellow
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SMILES
O=C(N(CCC1)C[C@]21CCN(CC3=CC=C(Cl)C(Cl)=C3)C2)NCC4=CC=C(C)C=C4
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Synonyms
GSK163
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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
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Most Recent
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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).
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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 -
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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.
Pureza y Documentación
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Ficha de datos (273 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
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 |
|---|---|---|---|---|---|
| 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 |
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