LY2090314

LY2090314 : Inhibitor of GSK3A, GSK3B

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe LY2090314 is in the process of SERP review.

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Information

GSK3A
GSK3B

Inhibitor

up to 100 nM

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: P49840

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 1.5 nM

Potency Assay: Biochemical assay

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

Target aliases:

Glycogen synthase kinase-3 alpha, GSK3A, GSK3A_HUM ...

DOI Reference: 10.1124/dmd.112.048488

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Screened against a panel of diverse Kinases: Kinase IC50 GSK-3β 0.0011 Cdk4 1.8 Cdk2 2.8 PKCβII 0.42 AKT1 >20 PDK-1 6.2 KDR >20 TGFβ-R2 1.2 hPKAβ >20 CAMKII >20 MLK7 >20 p38 >20

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Limited (not whole kinome) selectivity data and no direct cellular target engagement assay data are provided in the primary publication, which uses downstream phospho-tau as a readout. Therefore additional profiling of this molecule is advised before use as a chemical probe for the named targets. The short t 1/2 and rapid clearance of this molecule may be limiting for in vivo studies.

(last updated: 26 Feb 2023 )