CID 53469059 1-(5-(4-氨基-7-甲基-7H-吡咯并[2,3-d]嘧啶-5-基)-4-氟吲哚啉-1-基)-2-(6-甲基吡啶-2-基)乙酮
CAS 1337532-29-2 MFCD437532292
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- GSK2656157 is an ATP-competitive inhibitor of PERK enzyme activity with an IC50 of 0.9 nM. It is highly selective for PERK with IC50 values >100 nM against a panel of 300 kinases. GSK2656157 inhibits PERK activity in cells with an IC50 in the range of 10-30 nM as shown by inhibition of stress-induced PERK autophosphorylation, eIF2α substrate phosphorylation, together with corresponding decreases in ATF4 and CHOP proteins in multiple cell lines. Oral administration of GSK2656157 to mice shows a dose- and time-dependent pharmacodynamic response in pancreas as measured by PERK auto-phosphorylation.