GSK2850163 hydrochloride
Based on 7 publication(s) in Google Scholar
GSK2850163 hydrochloride 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.
For research use only. We do not sell to patients.
- CAS No.: 2319838-09-8
- Formula: C24H30Cl3N3O
- Molecular Weight:482.87
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) GSK2850163 hydrochloride
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.
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Biological Activity
IC50: 20 nM (IRE1α kinase activity), 200 nM (IRE1α RNase activity)[1]
GSK2850163 hydrochloride 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 can be reduced in a dose-dependent manner by GSK2850163 hydrochloride. Increasing concentrations of GSK2850163 hydrochloride are capable of reducing the increased XBP 1 transcriptional activity. Two additional kinases are weakly inhibited by GSK2850163 hydrochloride: 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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CAS No. 2319838-09-8
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Molecular Weight 482.87
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Formula C24H30Cl3N3O
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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.Cl
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Synonyms
GSK163 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
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 hydrochloride 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 hydrochloride 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 hydrochloride 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 -
Protocol
In the ADP-Glo assay, GSK2850163 hydrochloride’s potency toward pIRE1α kinase activity is measured as its inhibition of an intrinsic, slowing ATP hydrolysis activity. One hundred nanoliters of dimethylsulfoxide solution of GSK2850163 hydrochloride at various concentrations is added into a 384-well plate. The reaction is carried out with 5 nM pIRE1α and 60 mM ATP in 10 mL of 50 mM Hepes buffer, pH 7.5, containing 30 mM NaCl, 10 mM MgCl2, 1 mM DTT, 0.02% Chaps, and 0.01 mg/mL bovine serum albumin. The reaction is stopped after 2 hours by adding 5 mL of ADP-Glo reagent I, which also depletes the remaining ATP. Following 1-hour incubation, 5 mL of ADP-Glo reagent II is added into the reaction, which converts the ADP product into ATP to serve as the substrate for the coupled luciferin/luciferase reaction. After 30 minutes, the plate is read on a microplate imager[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 hydrochloride 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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSK2850163 hydrochloride Related Classifications
HY-U00459B Related Classifications
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