PERK-IN-6

Names

[ CAS No. ]:
1337532-14-5

[ Name ]:
PERK-IN-6

Biological Activity

[Description]:

PERK-IN-6 (Compound 5) is a PERK inhibitor with an IC50 of 2.5 nM[1].

[Related Catalog]:

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

[Target]

IC50: 2.5 nM (PERK)[1]


[In Vitro]

在 A549 细胞中,PERK-IN-6 (Compound 5) 抑制 thapsigargin 诱导的 PERK 自磷酸化,IC50 为 0.1-0.3 μΜ[1]。

[In Vivo]

SD 大鼠静脉注射 PERK-IN-6 (Compound 5) 后血液清除率为 10.5 mL/min/kg [1]。

[References]

[1]. Axten JM, et al. Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development. ACS Med Chem Lett. 2013 Aug 12;4(10):964-8.  

Chemical & Physical Properties

[ Molecular Formula ]:
C23H22N6O

[ Molecular Weight ]:
398.46