MilliporeSigma™ Calbiochem™ PERK Inhibitor II, GSK2656157

Description

PERK Inhibitor II, GSK2656157, CAS 1337532-29-2 is a cell-permeable, potent, ATP-competitive inhibitor of PERK/EIF2AK3 (IC50 = 0.9nM).

A cell-permeable pyrrolopyrimidinamine compound that acts as a potent, ATP-competitive EIF2AK3/PERK inhibitor (IC₅₀ = 0.9nM; [ATP] = 10μM), displaying ≥511-fold selectivity over HRI/EIF2AK1, BRK, PKR/EIF2AK2, and MEKK2 (IC₅₀ = 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 (IC₅₀ ≤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).

Specifications

• Color: White
• Description: 98% by HPLC
• Target Proteins: PERK
• Molecular Formula: C₂₃H₂₁FN₆O
• Solubility: DMSO
• Content And Storage: Protect from light
• Form: Powder
• Quantity: 5 mg