SGC-GSK3-1

SGC-GSK3-1 : Inhibitor of GSK3A and GSK3B

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe SGC-GSK3-1 is in the process of SERP review.

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Information

GSK3A
GSK3B

Inhibitor

up to 1 uM

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: P49840

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 1.0 nM

Potency Assay: Enzymatic assay

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

Target aliases:

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

DOI Reference: 10.1021/acschemneuro.3c00135

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): SGC-GSK3-1 was analyzed at 1 μM in the Eurofins DiscoverX scanMAX panel (403 wild-type (WT) human as well as several mutant and non-human kinases): SGC-GSK3-1 proved to be exquisitely selective compounds, binding to only five kinases with PoC < 10 at 1 μM.

Potency assay, off target (cells): 200-fold selectivity window is observed between GSK3β and DYRK1B when comparing NanoBRET cellular target engagement

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

This is a good probe, with high in vitro and in-cell potency, a clear selectivity profile within the family, and proven target engagement. The compound is also safe for neuron cells. There is a related compound that is suitable for studies that involve a closely related target, CDKL5. Data on selectivity outside of the family is unfortunately unavailable.

(last updated: 17 Jun 2024 )