Ruxolitinib

ATP-competitive inhibitor of JAK1, JAK2

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(3 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

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Information

Protein target names: JAK1, JAK2

Mechanism of action: ATP-competitive inhibitor

Recommended in-cell concentration:

5 nM - 1 uM

Primary References:

DOI - 10.1182/blood-2009-04-214957

Probe Availability:

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

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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 )