GSK2656157

GSK2656157 is an inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK, IC50 = 0.9 nM). It is selective for PERK over a panel of additional kinases. GSK2656157 blocks both stress-induced PERK autophosphorylation and eIF2alpha substrate phosphorylation and decreases levels of ATF4 and CHOP in multiple cell lines. It is orally bioavailable, suppressing PERK autophosphorylation in mouse pancreas and inhibiting the growth of multiple human tumor xenografts in mice. GSK2656157 inhibits caspase 1 activation in macrophage-like J774.1 cells, preventing LPS-induced IL-1beta production, through its effects on the PERK/eIF2alpha pathway.Formal Name: 1-[5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoro-2,3-dihydro-1H-indol-1-yl]-2-(6-methyl-2-pyridinyl)-ethanone. CAS Number: 1337532-29-2. Molecular Formula: C23H21FN6O. Formula Weight: 416.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml, Ethanol: 2 mg/ml. lambdamax: 287 nm. SMILES: NC1=NC=NC2=C1C(C3=CC=C4C(CCN4C(CC5=CC=CC(C)=N5)=O)=C3F)=CN2C. InChi Code: InChI=1S/C23H21FN6O/c1-13-4-3-5-14(28-13)10-19(31)30-9-8-16-18(30)7-6-15(21(16)24)17-11-29(2)23-20(17)22(25)26-12-27-23/h3-7,11-12H,8-10H2,1-2H3,(H2,25,26,27). InChi Key: PRWSIEBRGXYXAJ-UHFFFAOYSA-N.