PERK-IN-4-d3
PERK-IN-4-d3 is the deuterium labeled PERK-IN-4. PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR) -like endoplasmic reticulum kinase) inhibitor with an IC50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states[1].
Product Specifications
UNSPSC
12352005
Target
Isotope-Labeled Compounds; PERK
Type
Isotope-Labeled Compounds
Related Pathways
Cell Cycle/DNA Damage; Others
Field of Research
Cancer; Metabolic Disease; Neurological Disease
Solubility
10 mM in DMSO
Smiles
NC1=C(C2=NC=N1)C(C3=CC=C4C(CCN4C(CC5=CC(C(F)(F)F)=CC(F)=C5)=O)=C3)=CN2C([2H])([2H])[2H]
Molecular Formula
C24H16D3F4N5O
Molecular Weight
472.45
References & Citations
[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]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;55 (16) :7193-7207.
Shipping Conditions
Room temperature
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported
Available Sizes
Frequently Asked Questions
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