SGC-STK-17B-1

SGC-STK-17B-1 : Inhibitor of STK17B

Structure

SERP Rating

In Cells

(3 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.

Information

STK17B

Inhibitor

up to 1 uM

Additional Data

SGC Chemical Probe Collection

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: O94768

Target Class: Kinase

Target SubClass: CAMK

Potency: Kd

Potency Value: 34 nM

Potency Assay: KinaseSeeker Split Luciferase Assay

PDB ID for probe-target interaction (3D structure): 6Y6H

Target aliases:

Serine/threonine-protein kinase 17B, DRAK2, STK17B ...

DOI Reference: 10.1021/acs.jmedchem.0c01174

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

SGC-STK17B-1 was profiled in the KINOMEscan assay against of 403 wild-type kinases @ 1 mM, followed by Kd determination of potential off-targets at Eurofins. SGC-STK17B-1 shown >30 fold selective (Kd) against the closest off-targets STK17A/DRAK1, AURKB and CaMKK2.

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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

The availability of a highly similar, but inactive, analog is a big plus for this probe. Although 1uM is probably safe, I would recommend starting lower than 1uM. The NanoBRET IC50 for CAMKK2 is 2.4uM, so at 1uM in cells, there may be residual effects on this kinase, too.

(last updated: 19 Jun 2022 )

SERP Ratings

In Cell Rating

SERP Comments:

This probe appears to have exquisite selectivity for STK17B and is appropriate for use in cell-based studies. It has some off-target effects on CAMKK2 and CAMKK1, but the apparent Kd for these off-targets in live cells is > 10x that of STK17B. As such, using this probe at concentrations of up to 1 uM can ensure substantial target engagement for STK17B and much less (probably 30% or less) engagement of CAMKK off-targets. The recommendation for cell-based studies would be to do a dose-response that maxes out at 1 uM, as this is likely to be the range that correlates best with selective inhibition of STK17B within cells.

(last updated: 24 Aug 2022 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

This compound is recommended as a chemical probe. It is well characterised in vitro (KinaseSeeker) and in cell (NanoBRET). It also has all structural data.

(last updated: 23 May 2024 )