AMG PERK 44

AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy[1][2].

Product Specifications

CAS Number

[1883548-84-2]

UNSPSC

12352005

Target

Autophagy; PERK

Type

Reference compound

Related Pathways

Autophagy; Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/amg-perk-44.html

Concentration

10mM

Purity

99.67

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

O=C1N(C2=CC=CC=C2)N(C)C(C3=CC=CC=C3)=C1C(C4=CC=C(C)C(C5=CC=C6N=C(C)C=CC6=C5)=C4N)=O.[H]Cl

Molecular Formula

C34H29ClN4O2

Molecular Weight

561.07

References & Citations

[1]Smith AL, et al. Discovery of 1H-pyrazol-3 (2H) -ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK) . J Med Chem. 2015 Feb 12;58 (3) :1426-41.|[2]Roest G, et al. The ER Stress Inducer l-Azetidine-2-Carboxylic Acid Elevates the Levels of Phospho-eIF2α and of LC3-II in a Ca2+-Dependent Manner. Cells. 2018 Nov 30;7 (12) . pii: E239.