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GSK 2606414
- Soluble in DMSO
- MF: C24H20F3N5O
- MW: 451.44
Description
GSK 2606414 is a potent and selective first-in-class PERK/EIF2AK3 inhibitor with reported IC50 of 0.4 nM and more than 1000-fold selectivity over EIF2AK1/HRI and EIF2AK2/PKR. It shows oral bioavailability and blood-brain barrier penetration in preclinical studies.
PERK is an ER membrane kinase and a primary effector of the unfolded protein response, with roles in tumor growth, angiogenesis, proteostasis and neurodegenerative stress. GSK 2606414 is relevant for studying PERK-dependent ER stress signaling.
Key Features
- Potent PERK/EIF2AK3 inhibitor
- High selectivity over related eIF2α kinases
- Orally bioavailable and brain-penetrant in reported studies
- Blocks unfolded protein response signaling
Applications
- PERK (Protein kinase R-like Endoplasmic Reticulum Kinase) kinase assays
- ER stress and UPR research
- Tumor growth and angiogenesis models
- Neurodegeneration stress pathway studies
More Information
| Parent CAS No. | 1337531-36-8 |
|---|---|
| Chemical Name | 1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone |
| SMILES | C1C=C2N(C(=O)CC3C=C(C(F)(F)F)C=CC=3)CCC2=CC=1C1=CN(C)C2N=CN=C(N)C1=2 |
| MFCD | N.A. |
| InChi | InChI=1S/C24H20F3N5O/c1-31-12-18(21-22(28)29-13-30-23(21)31)15-5-6-19-16(11-15)7-8-32(19)20(33)10-14-3-2-4-17(9-14)24(25,26)27/h2-6,9,11-13H,7-8,10H2,1H3,(H2,28,29,30) |
| InChiKey | SIXVRXARNAVBTC-UHFFFAOYSA-N |
| CID | 53469448 |
| Short Description | PERK inhibitor |
References
- J.M. Axten et al. 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 PERK (...). J. Med. Chem. 2012, 55, 7193-7207.
- J.A. Moreno 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.
- List of publications using GSK 2606414 (Axon 2233) purchased from Axon Medchem
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