GNE-3511
Inhibitor of MAP3K12
Structure
In Cells
In Model Organisms
SERP ratings and comments
SERP Ratings
SERP Comments:
This is a relatively promiscuous inhibitor of DLK. As indicated by the published kinome profile, many kinases are >80% inhibited at 100 nM. Care must be exercised when attributing pharmacological observations to DLK inhibitors. I would recommend using other pharmacological interventions (e.g., URMC-099) and genetic interventions to validate studies using GNE-3511.
(last updated: 23 Jul 2021 )
SERP Ratings
SERP Comments:
GNE-3511 has been rigorously tested in kinase activity panels and for inhibition of closely related kinases. Biomarkers (p-c-Jun) suggest on-target activity in mouse studies.
(last updated: 29 Jul 2021 )
SERP Ratings
SERP Comments:
While this probe is a good tool for studying DLK inhibition in vitro and in vivo, there is some need to further understand selectivity, especially at higher doses and in a cellular context. Recommended concentration up to 50nM covers the IC50, but some phenotypes may require more inhibition.
(last updated: 25 Aug 2021 )