Cat. No. Name Size Price Add Cart
KI3697GSK26064145 mg$334
GSK260641425 mg$1456
GSK260641450 mg$2330

Chemical Characteristic

Product NameGSK2606414
CAS No.1337531-36-8
Molecular Weight 451.44
FormulaC24H20F3N5O
Smilesc1nc2c(c(n1)N)c(cn2C)c1cc2CCN(c2cc1)C(=O)Cc1cc(ccc1)C(F)(F)F
Chemical Structure

Biological activities

GSK2606414 is a drug that is the first selective inhibitor discovered for the enzyme protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK), which is involved in various processes relating to cancer and neurodegenerative disorders [1]. GSK2606414 was found to be a potent and selective inhibitor of PERK, with good oral bioavailability and blood-brain barrier penetration. GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed. In vitro, it can be used by 10?M[2].

References

[1] Axten JM, et al. Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-p yrrolo[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, 55(16):7193-7207.
[2] Moreno, J. A, et al. Oral Treatment Targeting the Unfolded Protein Response Prevents Neurodegeneration and Clinical Disease in Prion-Infected Mice. Science Translational Medicine.2013, 5 (206): 206ra138.

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