MilliporeSigma™ Calbiochem™ PERK Inhibitor II, GSK2656157

Description

• A cell-permeable pyrrolopyrimidinamine compound that acts as a potent, ATP-competitive EIF2AK3/PERK inhibitor (IC 50 = 0.9nM; [ATP] = 10μM), displaying ≥511-fold selectivity over HRI/EIF2AK1, BRK, PKR/EIF2AK2, and MEKK2 (IC 50 = 460, 822, 905, and 954 nM, respectively) and much reduced or little activity toward more than 300 other kinases
• Potently prevents ER stress-induced enhancement of PERK and eIF2α phosphorylation as well as ATF4 and CHOP upregulation in human BxPC3 and murine LL/2 cultures in vitro (IC 50 ≤30nM; 1 h drug preincubation prior to 6 h 1μM Thapsigargin treatment, Cat
• No
• 586005) and exhibits antitumor efficacy against 3 pancreas and 1 multiple myeloma xenografts in mice (54-110% tumor growth inhibition; 150mg/kg/12 h via p.o.) in vivo
• More selective than GSK2606414 (Cat
• No
• 516535).