GSK2850163

Product Name: GSK2850163
CAS No.: 2121989-91-9
Chemical Name: GSK2850163
Synonyms: GSK2850163;GSK2850163, 10 mM in DMSO;inhibit,IRE1,GSK 2850163,Inhibitor,Inositol requiring enzyme 1,GSK2850163,GSK-2850163;2,7-Diazaspiro[4.5]decane-7-carboxamide, 2-[(3,4-dichlorophenyl)methyl]-N-[(4-methylphenyl)methyl]-, (5R)-
CBNumber: CB23386486
Molecular Formula: C24H29Cl2N3O
Formula Weight: 446.41
MOL File: 2121989-91-9.mol

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GSK2850163 Property

Boiling point:: 625.6±55.0 °C(Predicted)
Density: 1.28±0.1 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: DMSO : 67.5 mg/mL (151.21 mM);Water : < 0.1 mg/mL (insoluble)
form: oil
pka: 13.81±0.20(Predicted)
color: colorless to light yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1684
Product name: GSK2850163
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $105
Updated: 2023/06/20

Sigma-Aldrich

Product number: SML1684
Product name: GSK2850163
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $424
Updated: 2023/06/20

ChemScene

Product number: CS-0039356
Product name: GSK2850163
Purity: 98.50%
Packaging: 5mg
Price: $80
Updated: 2021/12/16

ChemScene

Product number: CS-0039356
Product name: GSK2850163
Purity: 98.50%
Packaging: 10mg
Price: $140
Updated: 2021/12/16

ChemScene

Product number: CS-0039356
Product name: GSK2850163
Purity: 98.50%
Packaging: 25mg
Price: $290
Updated: 2021/12/16

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GSK2850163 Chemical Properties,Usage,Production

Biochem/physiol Actions

GSK2850163 is a highly selective inhibitor of inositol requiring enzyme-1 alpha (IRE1α) with dual activity: it inhibits IRE1α kinase activity with an IC50 value of 20 nM and RNase activity with an IC50 value of 200 nM. IRE1α is a dual serine/threonine-protein kinase/endoribonuclease with two enzymatic domains: a trans-autophosphorylation domain and and endoribonuclease (RNase) domain. When activated, usually in response to endoplasmic reticulum (ER) stress such as the unfolded protein response (UPR), IRE1α oligomerizes and activates mRNA splicing of adaptive XBP1 transcription factor, which upregulates ER chaperones and ER associated degradation (ERAD) genes that promote degradation of ER unfolded proteins and facilitate recovery from ER stress. However, if ER stress is too high or chronic, IRE1α is hyperactivated, increasing many ER mRNAs, resulting in apoptosis. GSK2850163 interacts with IRE1α catalytic residues Lys599 and Glu612, displacing the kinase activation loop to the inactive DFG-out conformation. The rearrangement of the kinase domain-dimer interface also results in the RNAse domains rotating away from each other, inhibiting the RNase activity.

GSK2850163 Preparation Products And Raw materials

Raw materials

Preparation Products

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GSK2850163 Suppliers

CHINA 15 United States 4 Global 19

Sigma-Aldrich

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2121989-91-9, GSK2850163Related Search:

GSK2850163

2,7-Diazaspiro[4.5]decane-7-carboxamide, 2-[(3,4-dichlorophenyl)methyl]-N-[(4-methylphenyl)methyl]-, (5R)-

inhibit,IRE1,GSK 2850163,Inhibitor,Inositol requiring enzyme 1,GSK2850163,GSK-2850163

GSK2850163, 10 mM in DMSO

2121989-91-9