PERK-IN-4

Names

[ Name ]:
PERK-IN-4

[Synonym ]:
Ethanone, 1-[5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoromethyl)phenyl]-
1-[5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-fluoro-5-(trifluoromethyl)phenyl]ethanone
GSK PERK Inhibitor

Biological Activity

[Description]:

PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states[1].

[Related Catalog]:

Research Areas >> Cancer

Research Areas >> Metabolic Disease

Signaling Pathways >> Cell Cycle/DNA Damage >> PERK

Research Areas >> Neurological Disease

[Target]

IC50: 0.3 nM (PERK)[1]

[References]

[1]. Axten JM, 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 protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem. 2012;55(16):7193-7207.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
710.9±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₄H₁₉F₄N₅O

[ Molecular Weight ]:
469.434

[ Flash Point ]:
383.7±32.9 °C

[ Exact Mass ]:
469.152588

[ PSA ]:
77.04000

[ LogP ]:
4.42

[ Vapour Pressure ]:
0.0±2.3 mmHg at 25°C

[ Index of Refraction ]:
1.660

Related Compounds

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