STO609

Reagent Authentication Certificate:

Chemical Probes Portal STO609.pdf

Protein target name:

CAMKK1, CAMKK2

Mechanism of action:

ATP-competitive inhibitor

Recommended Concentration for use in cells:

Up to 300 nM

Probe Availability

Tocris (1173022-21-3)

Abcam (52029-86-4)

MedChem Express (52029-86-4)

Cayman (1173022-21-3)

MilliporeSigma (STO609 acetic acid)

Probe Information

Target and Probe Information

Target Details

Target class:

Protein kinase

Subclass:

Other

HUGO ID:

HGNC:1469 HGNC:1470

Entrez gene ID:

84254 10645

UNIPROT ID:

Q8N5S9 Q96RR4

Target alias:

CAMKKA, CAMKK, CAMKKB, calcium/calmodulin dependent protein kinase - kinase 1, calcium/calmodulin dependent protein kinase - kinase 2

Probe Details

Chemical Probes Portal ID:

CPP109

Probe alias:

STO 609, NCGC00025213-01, AC1MRG00, GTPL5274, ZINC9295, STO-609

PubChem CID:

3467590

ChEMBL ID:

CHEMBL1182777

SMILES string:

C1=CC=C2C(=C1)N=C3N2C(=O)C4=CC=CC5=C(C=CC3=C54)C(=O)O

InChi Key:

MYKOWOGZBMOVBJ-UHFFFAOYSA-N

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

0.25 uM (CAMKK1) and 0.047 uM (CAMKK2)

Potency assay:

IC50s in in vitro kinase assays: CAMKK1 0.38 uM. CAMKK2 0.12 uM

Off target activity

Potency assay (off target):

100-fold or more selective compared with CAMK1, CAMK4, CAMK2 gamma, MYLK, PRCK, and PRKACA

In cell validation

On target activity in cells

Potency assay (cells):

In HeLa cells transfected with CAMK, STO609 dose-dependently inhibited CAMK substrate phosphorylation.

Target engagement assay (cells):

Indirect: inhibition of protein substrate phosphorylation

Primary Reference

Reference (doi):

10.1074/jbc.M201075200

Reference (PMID):

11867640

STO609

Probe Availability

Probe Information

Target Details

CAMKKA, CAMKK, CAMKKB, calcium/calmodulin dependent protein kinase - kinase 1, calcium/calmodulin dependent protein kinase - kinase 2

Probe Details

In vitro validation

In cell validation

Primary Reference

Supporting Organizations

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STO609

Probe Availability

Probe Information

Target Details

CAMKKA, CAMKK, CAMKKB, calcium/calmodulin dependent protein kinase - kinase 1, calcium/calmodulin dependent protein kinase - kinase 2

Probe Details

In vitro validation

In cell validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?