AZ2858

AZ2858 : Inhibitor of GSK3B

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe AZ2858 is in the process of SERP review.

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Information

GSK3B

Inhibitor

up to 1 uM

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: P49841

Target Class: Kinase

Target SubClass: CMGC

Potency: Ki

Potency Value: 4.9 nM

Potency Assay: Biochemical Assay

PDB ID for probe-target interaction (3D structure): 4ACD

Target aliases:

Glycogen synthase kinase-3 beta, GSK3B, GSK3B_HUMA ...

DOI Reference: 10.1021/jm201724m

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): AZD2858 was evaluated for pan-kinase selectivity (10 μM). The compound shows a good overall selectivity versus 26 kinases. CDK2 Ki 510 nM, corresponding to a 110-fold selectivity versus CDK2.

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

This is a potent compounds (4.9 nM in vitro) and a decent selectivity of 110 fold in the panel tested. However, the selectivity has only been assessed versus 26 kinases. Using an orthogonal probe is therefore essential when using this compound. Tau phosphorylation and a western blot have been performed for validation of reactivity of compound 18. Additionally, permeability and solubility are reported and BBB-permeability have been measured.

(last updated: 17 Jun 2024 )

Portal Comments

Note that AZ2858 was not specifically assessed for its binding to the related GSK3A

(last updated: 24 Jan 2023)