Ruxolitinib
ATP-competitive inhibitor of JAK1, JAK2
Structure
In Cells
In Model Organisms
Information
Protein target names: JAK1, JAK2
Mechanism of action: ATP-competitive inhibitor
In Vitro Validations
DOI Reference: 10.1182/blood-2009-04-214957
In Cell Validations
In Vivo Data
Reagent authentication certificate:
SERP ratings and comments
SERP Ratings
(last updated: 20 May 2016 )
SERP Ratings
Comments:
This compound inhibits JAK1 IC50 7 nM (1 mM ATP) and JAK2 IC50 9 nM (1 mM ATP) equally well. Because either JAK1 or JAK2 can be a part of any receptor pairing in any in vitro or in vivo setting, this probe evaluates the effect of pan-JAK inhibition.
(last updated: 31 May 2016 )
SERP Ratings
Comments:
Validation for this compound is high. No significant inhibtion was observed in a panel of 26 kinases when tested at a concentration 100-fold higher than the IC50 observed for JAK1/2, though the modest selectivity against TYK2 is worth noting.
(last updated: 24 Aug 2016 )