STO609

ATP-competitive inhibitor of CAMKK1, CAMKK2

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

CAMKK1
CAMKK2

ATP-competitive inhibitor

Probe Availability:

In Vitro Validations

Uniprot ID: Q8N5S9

Target Class: Kinase

Target SubClass: Other

Potency: Ki

Potency Value: 250 nM

Potency Assay: Autophosphorylation of CaM-KKα and -β

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

Target aliases:

Calcium/calmodulin-dependent protein kinase kinase ...

DOI Reference: 10.1074/jbc.M201075200

Uniprot ID: Q8N5S9

Target Class: Kinase

Target SubClass: Other

Potency: IC 50

Potency Value: 380 nM

Potency Assay: in vitro kinase assays

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

Target aliases:

Calcium/calmodulin-dependent protein kinase kinase ...

DOI Reference: 10.1074/jbc.M201075200

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): 100-fold or more selective compared with CAMK1, CAMK4, CAMK2 gamma, MYLK, PRCK, and PRKACA

Probe Selectivity in Vitro:

STO-609 is highly selective for CaM-KK without any significant effect on the downstream CaM kinases (CaM-KI and -IV)

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SERP ratings and comments

SERP Ratings

In Cell Rating

(last updated: 29 Aug 2016 )

SERP Ratings

In Cell Rating

(last updated: 29 Aug 2016 )

SERP Ratings

In Cell Rating

(last updated: 29 Aug 2016 )