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.