GSK2656157

GSK2656157 : Inhibitor of EIF2AK3

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe GSK2656157 is in the process of SERP review.

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Information

EIF2AK3

Inhibitor

100 nM to 1 uM

Probe Availability:

In Vitro Validations

Uniprot ID: Q9NZJ5

Target Class: Kinase

Target SubClass: Ser/Thr Kinase

Potency: IC50

Potency Value: 0.8 nM

Potency Assay: Phosphorylation of human eIF2α

PDB ID for probe-target interaction (3D structure): 4M7I

Target aliases:

Eukaryotic translation initiation factor 2-alpha k ...

DOI Reference: 10.1021/ml400228e

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Kinase selectivity was evaluated using 27 kinases at GSK as well as a panel of 300 kinases at Reaction Biology Corp; weak P450 inhibitory potency

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 23 Oct 2022 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

GSK2656157 is selective inhibitor of PERK kinase (EIF2AK3) that binds the nucleotide pocket. In terms of selectivity in binding potency, it is at least 500-fold selective over other members of the EIF2AK family, with minimal inhibition of other off kinases when surveyed in a broad panel (300 kinases). It is potent in cells, demonstrating clear inhibition of PERK autophosporylation at 100nM or less, but can be used at concentrations up to 1uM meaningful off target effects. It is also bioavailable and can be used in multiple animal models such as the mouse, the rat, and the dog via either intravenous or oral routes. GSK2656157 should provide a valuable tool for the study of PERK in the context of various cancers or other disease contexts where inhibition of angiogenesis is desired.

(last updated: 26 Oct 2022 )