A selective inhibitor of PERK (IC50 = 0.9 nM); blocks both stress-induced PERK autophosphorylation and eIF2α substrate phosphorylation and decreases levels of ATF4 and CHOP in multiple cell lines

GSK2656157 – 5 mg

Brand:
Cayman
CAS:
1337532-29-2
Storage:
-20
UN-No:
Non-Hazardous - /

GSK2656157 is an inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK; IC50 = 0.9 nM).{32772,32773} It is selective for PERK over a panel of additional kinases.{32772} GSK2656157 blocks both stress-induced PERK autophosphorylation and eIF2α substrate phosphorylation and decreases levels of ATF4 and CHOP in multiple cell lines.{32772} It is orally bioavailable, suppressing PERK autophosphorylation in mouse pancreas and inhibiting the growth of multiple human tumor xenografts in mice.{32772,32773} GSK2656157 inhibits caspase 1 activation in macrophage-like J774.1 cells, preventing LPS-induced IL-1β production, through its effects on the PERK/eIF2α pathway.{32771}  

 

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Description

A selective inhibitor of PERK (IC50 = 0.9 nM); blocks both stress-induced PERK autophosphorylation and eIF2α substrate phosphorylation and decreases levels of ATF4 and CHOP in multiple cell lines

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

Synonyms: 

Molecular weight: 416.5

CAS: 1337532-29-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling

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