GSK2656157

GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR) -like endoplasmic reticulum kinase (PERK) with an IC50 of 0.9 nM.

Product Specifications

CAS Number

[1337532-29-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Autophagy; PERK

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/GSK2656157.html

Purity

99.66

Solubility

DMSO : 8.33 mg/mL (ultrasonic)

Smiles

CC1=CC=CC(CC(N2CCC3=C2C=CC(C4=CN(C)C5=NC=NC(N)=C54)=C3F)=O)=N1

Molecular Formula

C23H21FN6O

Molecular Weight

416.45

Precautions

H302, H315, H319, H335

References & Citations

[1]Atkins C, et al. Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res. 2013 Mar 15;73 (6) :1993-2002.|[2]Krishnamoorthy J, et al. Evidence for eIF2α phosphorylation-independent effects of GSK2656157, a novel catalytic inhibitor of PERK with clinical implications. Cell Cycle. 2014 Mar 1;13 (5) :801-6.|[3]Ando T, et al. GSK2656157, a PERK inhibitor, reduced LPS-induced IL-1β production through inhibiting Caspase 1 activation in macrophage-like J774.1 cells. Immunopharmacol Immunotoxicol. 2016 Aug;38 (4) :298-302.|[4]Zhao Q, et al. Thioredoxin-interacting protein links endoplasmic reticulum stress to inflammatory brain injury and apoptosis after subarachnoid haemorrhage. J Neuroinflammation. 2017 May 11;14 (1) :104.