Chemical Probes logo

HG-9-91-01

ATP-competitive inhibitor of SIK1, SIK2, SIK3

Structure

Information

  • SIK1
  • SIK2
  • SIK3
  • ATP-competitive inhibitor

In Vitro Validations

Uniprot ID: P57059
Target Class: Kinase
Target SubClass: CAMK
Potency: IC50
Potency Value: 0.92 nM
Potency Assay: In vitro kinase assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Serine/threonine-protein kinase SIK1, SNF1LK, SIK, ...

DOI Reference: 10.1073/pnas.1215450109

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency end-point : IC50 NUAK2 145 nM
Potency assay (off target): HG-9-91-01 was also active against SRC, LCK, YES, BTK, FGFRs, and Ephrin receptors. It was not active against any AMPK family kinases.
I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

In a limited panel (108 kinases), HG-9-91-01 inhibited several kinases (including SFKs) to a similar extent as the SIKs at 100 nM. Given the limited selectivity information available, use caution when using this probe. 

(last updated: 21 Dec 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

This probe is useful in cells when assayed alongside other, also not uniquely selective SIK inhibitors. Use in animals will require additional in vivo profiling (e.g., PK data).

(last updated: 20 Jan 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

This compound showed several off-targets in a very limited kinase panel of 108 kinases with a concentration of 100 nM. To use this compound as a probe, more detailed selectivity data should be determined in order to avoid measuring off-target effects. As a pan-SIK inhibitor this compound is not appropriate to study the effects associated with a single isoform.

(last updated: 9 Feb 2017 )