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PERK-IN-2

Names

[ CAS No. ]:
1337531-83-5

[ Name ]:
PERK-IN-2

Biological Activity

[Description]:

PERK-IN-2 is a potent PERK inhibitor with an IC50 of 0.2 nM[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> PERK

[Target]

IC50: 0.2 nM (PERK)[1]


[In Vitro]

PERK-IN-2 (0.03-0.3 μM; 2 hours) inhibits PERK autophosphorylation in A459 cells with IC50 value ranging from 0.03−0.1 μM[1]. Cell Viability Assay[1] Cell Line: A459 cells Concentration: 0.03 μM, 0.1 μM, 0.3 μM Incubation Time: 2 hours Result: Inhibited PERK autophosphorylation in A459 cells.

[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 Aug 23;55(16):7193-207.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H18F3N5O

[ Molecular Weight ]:
437.42

Related Compounds