GSK583

ATP competitive inhibitor of RIPK2

Structure

Information

Protein target names: RIPK2

Mechanism of action: ATP competitive inhibitor

Recommended in-cell concentration:
200 nM

In Vitro Validations

Uniprot ID: O43353
Target Class: Kinase
Target SubClass: TKL
Potency: IC50
Potency Value: 5 nM
Potency Assay: A fluorescent polarization based binding assay was developed to quantitate interaction of novel test compounds at the ATP binding pocket of RIPK2 by competition with a fluorescently labeled ATP competitive ligand.
PDB ID for probe-target interaction (3D structure): 5J7B
Structure-activity relationship: See J. Med. Chem. 2016, 59, 4867−4880.
Target aliases:
Receptor-interacting serine/threonine-protein kina ...

DOI Reference: 10.1021/acs.jmedchem.6b00211

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 17 Mar 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 27 Mar 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

GSK583 is a potent and selective molecule for the inhibition of RIP2 kinase, and it could be useful in probing the role of NOD1 and NOD2 in the pathogenesis of inflammatory disease. The compound has a reasonable profile for in vivo studies in rodents but falls short for human studies due to low exposure and safety concerns related to both hERG and CYP3A4.

(last updated: 29 Mar 2017 )