SGK1-IN-1

SGK1-IN-1 : Inhibitor of SGK1

Structure

SERP Rating

In Cells

(2 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.

Probe SGK1-IN-1 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

SGK1

Inhibitor

up to 1 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: O00141

Target Class: Kinase

Target SubClass: AGC

Potency: IC50

Potency Value: 1 or 41 nM

Potency Assay: enzymatic potency using 10 or 500 uM ATP, respectively

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

Target aliases:

Serine/threonine-protein kinase Sgk1, SGK, SGK1, S ...

DOI Reference: 10.1021/ml5003376

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: SGK2 128 nM SGK3 3100 nM Assessed against a panel of 60 Kinases with no inhibition higher than 50% at 1 uM.

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

Compound is ATP-competitive and binds to target and displays selectivity against kinase targets and anti-targets through profiling. The compound suffers incredibly poor aqueous solubility which limits its application to cell work. Significant differences in drop-offs between biochemical vs cell potency observed with analogues is not explained. There is no evidence presented that the control experiment has been completed i.e. GSK3b phosphorylation with AKT inhibitor alone therefore it is not clear that the observed effect is solely due to SGK inhibition alone. Use of an orthogonal probe desirable.

(last updated: 22 Nov 2023 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

There are no available probes for SGK1 with comparably high potency. A direct target engagement is not really shown, but phosphorylation of GSK3beta has been described. The compound has only been tested in a small kinase panel (of 60 kinases) with one off-target describes (AMP dependent kinase with IC50 of 1 µM ), data for SGK2 and SGK3 were not found. The compound shows very low solubility: <0.001 mg/mL. Further profiling would be necessary to recommend this compound as a chemical probe.

(last updated: 17 Jun 2024 )