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Product name : GSK-2606414
Item : CR1798
Price : 200mg, $945; 500mg, $1785
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Additional Information :  We offer significant discount for bulky quantity order,Please ask price and availability of other quantities
CAS : 1337531-36-8
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Details:
 Chemical Information
M.Wt 451.44 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C24H20F3N5O
CAS No 1337531-36-8
Solubility

DMSO



Biological Activity of GSK2606414

 

GSK2606414 is an orally available, potent, and selective PERK inhibitor with an IC50 of 0.4 nM.
IC50 Value: 0.4 nM [1]
Target:PERK
GSK2606414 inhibits PERK activation in cells and inhibits the growth of a human tumor xenograft in mice. Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states [1]. It is implicated that PERK plays an important role in tumorigenesis and cancer cell survival.
 

 

[1]. Axten JM, Medina JR, Feng Y, Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem. 2012 Aug 23;55(16):7193-207.


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