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GSK2850163

GSK2850163 Struktur
2121989-91-9
CAS-Nr.
2121989-91-9
Englisch Name:
GSK2850163
Synonyma:
GSK2850163;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
Summenformel:
C24H29Cl2N3O
Molgewicht:
446.41
MOL-Datei:
2121989-91-9.mol

GSK2850163 Eigenschaften

Siedepunkt:
625.6±55.0 °C(Predicted)
Dichte
1.28±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
L?slichkeit
DMSO : 67.5 mg/mL (151.21 mM);Water : < 0.1 mg/mL (insoluble)
Aggregatzustand
oil
pka
13.81±0.20(Predicted)
Farbe
colorless to light yellow

Sicherheit

GSK2850163 Chemische Eigenschaften,Einsatz,Produktion Methoden

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 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


GSK2850163 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 15)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000
marketing@targetmol.com United States 32161 58
InvivoChem
+1-708-310-1919 +1-13798911105
sales@invivochem.cn United States 6391 58
TargetMol Chemicals Inc.

support@targetmol.com United States 38631 58
Aladdin Scientific
+1-+1(833)-552-7181
sales@aladdinsci.com United States 52924 58
Sigma-Aldrich 021-61415566 800-8193336
orderCN@merckgroup.com China 51456 80
ChemeGen(Shanghai) Biotechnology Co.,Ltd. 18818260767
sales@chemegen.com China 11218 58
Guangzhou Younan Technology Co., Ltd 020-82000279 18988968278
sales@ubiochem.com China 4297 58
Shanghai hongqu biomedical technology co. LTD 88888888888
hongquchem@qq.com China 5132 58
Chunchuang (Wuhan) Technology Co., Ltd 15342225168
yutianchun2007@126.com China 10003 58
InvivoChem 13549236410
sales@invivochem.cn China 6753 58

  • 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
  • 2121989-91-9
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