AZ191

Inhibitor of DYRK1B

Structure

Information

Protein target names: DYRK1B

Mechanism of action: Inhibitor

In Vitro Validations

Uniprot ID: Q9Y463
Target Class: Protein kinase
Target SubClass: CMGC
Potency: IC50
Potency Value: 17 nM
Potency Assay: in vitro radioactivity-based substrate phosphorylation assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Dual specificity tyrosine-phosphorylation-regulate ...

In Cell Validations

In Vivo Data

No in Vivo Validations

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SERP ratings and comments


SERP Ratings

In Cell Rating

Comments:

This compound is too promiscuous kinome-wide to be useful as a cellular inhibitor of DYRK1B.

(last updated: 20 May 2016 )

SERP Ratings

In Cell Rating

Comments:

AZ191 is claimed to have 5-10x selectivity over DYRK1A and >100x over DYRK2. This molecule has been tested against >400 kinases at 1 uM and only hits 9 of them. A range of cellular effects are reported as well as cellular markers of activity. This tool is recommended for use in preference to the older, less selective harmine and derivatives.

(last updated: 26 May 2016 )

SERP Ratings

In Cell Rating

Comments:

Concentrations higher than a few micromolar are likely to inhibit other kinases.

(last updated: 15 Jun 2016 )