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AMG PERK 44

CAT: 0804-HY-12661A-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-12661A-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
No Development Reported