WH-4-023

Inhibitor of LCK, SRC

Structure

Information

Protein target names: LCK SRC

Mechanism of action: Inhibitor

In Vitro Validations

Uniprot ID: P06239
Target Class: Kinase
Target SubClass: TK
Potency: IC 50
Potency Value: 0.6 nM
Potency Assay: Kinase enzymatic activity
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Tyrosine-protein kinase Lck, LCK, LCK_HUMAN, LSK, ...

DOI Reference: 10.1021/jm060435i

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 14 Jun 2016 )

SERP Ratings

In Cell Rating

Comments:

This is a very promiscuous tyrosine kinase inhibitor.

(last updated: 15 Jun 2016 )

SERP Ratings

In Cell Rating

Comments:

WH-4-023 is compound 28 in the referenced work. However, this compound is one of a number synthesised, and the actual paper discusses detailed profiling of a compound 43. This later compound is more potent in cells, is better characterised in terms of its kinase selectivity, and has in vivo data presented (PK and PD). It is not clear how compound 28 has received the designation of WH-4-023 in preference to the true subject of the paper (Compound 43). In the absence of any detailed profiling of 28 it cannot be recommended as a suitable probe. This is also not a recommendation of compound 43 - that should be considered separately. Both compounds, and the series in general would appear to be potent pan SRC/LCK-family inhibitors, and possess a number of other activities, including a range of sub uM kinase activities not always associated with SRC-family inhibition. Much more selective probes for LCK exist, see for example A-770041 from Abbott.

(last updated: 23 Jun 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

This appears to be non-selective versus Src. Further kinase profiling is needed prior to recommendation as a probe for Lck.

(last updated: 27 Jun 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

Poor bioavailability hampers use of WH-4-023 as in vivo probe in mice.

(last updated: 29 Jun 2016 )