Inhibitor of NUAK1, NUAK2
Protein target names: NUAK1, NUAK2
Mechanism of action: Inhibitor
In Vitro Validations
DOI Reference: 10.1042/BJ20131152
In Cell Validations
In Vivo Data
No in Vivo Validations
Reagent authentication certificate:
SERP ratings and comments
No available PK or toxicology data; no way to judge whether or not it should be utilized in vivo. The probe is selective and has a target not well addressed by other molecules. Further work on physiochemistry, pharmacokinetics, and toxicology scouting could prove the probe useful (or disqualify for further use).
(last updated: 6 May 2016 )
This appears to be a highly selective NUAK1 inhibitor without significant off-target actions at 140 other tested kinases. There are no data available for potential off-target actions at other druggable targets (e.g., GPCRs, ion channels and so on).
(last updated: 15 Jun 2016 )
The compound has good kinase selectivity, but the cellular activity is not at the level I would consider useful for a bona fide probe (<1 uM). The authors have highlighted a few more potent compounds that could be used in parallel. They suffer from a worse kinome profile. This compound has excellent kinase selectivity but is only weekly active in cells.
(last updated: 17 Jun 2016 )