GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 80 mg/mL|
|Related PERK Products|
WAY-354896 is a Dual activator of Protein Kinase R (PKR) and Protein Kinase R-Like Kinase (PERK).
CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.
ISRIB is a potent and selective PERK inhibitor with IC50 of 5 nM.
trans-ISRIB is a integrated stress response (ISR) inhibitor.
Salubrinal is a selective inhibitor of eIF2α dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM.
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