Ruxolitinib

ATP-competitive inhibitor of JAK1, JAK2

Structure

Information

Protein target names: JAK1 JAK2

Mechanism of action: ATP-competitive inhibitor

Recommended in-cell concentration:
5 nM - 1 uM

In Vitro Validations

Uniprot ID: P23458
Target Class: Kinase
Target SubClass: TK
Potency: IC 50
Potency Value: 3.3 nM
Potency Assay: Kinase Enzymatic assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Tyrosine-protein kinase JAK1, JAK1B, JAK1A, JAK1, ...

DOI Reference: 10.1182/blood-2009-04-214957

In Cell Validations

In Vivo Data

Reagent authentication certificate: PDF image

I have extra information to add

SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 20 May 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

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

In Cell Rating
In Model Organisms

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 )