Catalog No.: PC-49643Not For Human Use, Lab Use Only.
GSK2656157 (GSK 2656157) is a potent, selective and ATP-competitive inhibitor of PERK with biochemical IC50 of 0.9 nM and cellular p-PERK IC50 of 30 nM.
GSK2656157 (GSK 2656157) is a potent, selective and ATP-competitive inhibitor of PERK with biochemical IC50 of 0.9 nM and cellular p-PERK IC50 of 30 nM.
GSK2656157 shows selectivity (>500-fold) over HRI, PKR, and GCN2, other members of the EIF2AK family, and high IC50 values (>100 nM) against a panel of 300 kinases.
GSK2656157 inhibits stress-induced PERK autophosphorylation, eIF2α substrate phosphorylation, together with corresponding decreases in ATF4 and CAAT/enhancer binding protein homologous protein (CHOP) in multiple cell lines.
Oral administration of GSK2656157 to mice shows a dose- and time-dependent pharmacodynamic response in pancreas as measured by PERK autophosphorylation.
GSK2656157 exhibited antitumor effect in multiple human tumor xenografts growth in mice.
