AZ191

Inhibitor of DYRK1B

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(0 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.

Information

DYRK1B

Inhibitor

Probe Availability:

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

Off-Target Selectivity Assesments

Potency end-point : IC50 DYRK1A 88 nM, DYRK2 1,890 nM

Potency assay (off target): In vitro radioactivity-based substrate phosphorylation assay

Probe Selectivity in Vitro:

In Kinomescan (DiscoverX) assessing >400 kinases, there were only 8 non-mutated kinase hits at 1 uM (CIT, DRAK1, DYRK1A, MEK5, MKNK2, PRKD2, RPS6KA4, YSK4).

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP 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

SERP 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

SERP Comments:

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

(last updated: 15 Jun 2016 )