SGK3-PROTAC1

SGK3-PROTAC1 : Degrader (PROTAC) of SGK3

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 ratings)

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Probe SGK3-PROTAC1 is in the process of SERP review.

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Information

SGK3

Degrader (PROTAC)

300 nM, up to 3 uM
Reviewer recommended concentration: 300 nM to ensure selective degradation

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q96BR1

Target Class: Kinase

Target SubClass: AGC

Potency: IC50

Potency Value: 300 nM

Potency Assay: Biochemical assay (radioactive filter binding assay using 33P ATP)

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

Target aliases:

Serine/threonine-protein kinase Sgk3, SGKL, CISK, ...

DOI Reference: 10.1021/acschembio.9b00505

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Dundee Kinase panel (140 targets) at 1 µM: Closest off-targets are [% activity remaining] SGK1 (34), RPS6KB1 (S6K1) (19); Biochemical assay: RPS6KB1 (IC50 = 1.8 µM), SGK1 (IC50 = 220 nM).

Potency assay, off target (cells): Proteomic analysis of HEK293 cells: clean

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

Excellent probe to study the biology of SGK3 at the concentration where degradation is driven . High selectivity against other member of the same family. There is modest degradation of S6K1 at concentrations between 1-10 uM which should be taken into account. Use of the probe at a concentration 0.3 uM is probably optimal to ensure selectivity of degradation.

(last updated: 9 Apr 2024 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

A specific Dmax value would be nice to have.

(last updated: 31 Oct 2024 )