DCLK1-IN-1

DCLK1-IN-1 : Inhibitor of DCLK1, DCLK2

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Information

DCLK1
DCLK2

Inhibitor

up to 1 uM

Probe Availability:

In Vitro Validations

Uniprot ID: O15075

Target Class: Kinase

Target SubClass: CAMK

Potency: Kd

Potency Value: 109 nM

Potency Assay: ITC

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Serine/threonine-protein kinase DCLK1, KIAA0369, D ...

DOI Reference: 10.1038/s41589-020-0506-0

Uniprot ID: O15075

Target Class: Kinase

Target SubClass: CAMK

Potency: IC50

Potency Value: 9.5 nM

Potency Assay: DCLK1 KINOMEscan binding assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Serine/threonine-protein kinase DCLK1, KIAA0369, D ...

DOI Reference: 10.1038/s41589-020-0506-0

Uniprot ID: O15075

Target Class: Kinase

Target SubClass: CAMK

Potency: IC50

Potency Value: 57.2 nM

Potency Assay: 33P-ATP DCLK1 kinase assay. Assays were performed at an ATP concentration of 50 μM (Km)

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Serine/threonine-protein kinase DCLK1, KIAA0369, D ...

DOI Reference: 10.1038/s41589-020-0506-0

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): KINOMEscan profiling at a concentration of 1 μM t across a panel of 489 human kinases. DCLK1-IN-1 exclusively inhibited DCLK1 and DCLK2 to below 10% of the control signal, while DCLK1-NEG did not inhibit any kinases using this cutoff.

Potency assay, off target (cells): Kinativ: DCLK1-IN-1 significantly inhibited DCLK1, and weakly inhibited ERK5, in PATU-8988T cell lysates and live cells. DCLK1-NEG did not inhibit any kinases under these conditions.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

DCLK1-IN-1 is high quality chemical probe suitable for in vitro as well as in vivo experiments to study DCLK1 and DCLK2 protein kinases. Its high kinome-wide selectivity was confirmed by testing at 1 uM concentration against large panel of protein kinases, while the closest off target (HIPK1) showed only 44 % residual activity. Potent in vitro and in cellulo activity was well documented using several complementary assays. In addition, the probe is accompanied by a structurally very similar negative control DCLK-NEG (contains only additional methyl group), which was also well characterized. DCLK1-IN-1 exhibits good pharmacokinetic profile and no obvious adverse effects up to 100 mg/kg in mice.

(last updated: 21 Feb 2023 )