calcium/calmodulin dependent protein kinase kinase 2 | Meta subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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calcium/calmodulin dependent protein kinase kinase 2

Target not currently curated in GtoImmuPdb

Target id: 1957

Nomenclature: calcium/calmodulin dependent protein kinase kinase 2

Abbreviated Name: CAMKK2

Family: Meta subfamily

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 588 12q24.2 CAMKK2 calcium/calmodulin dependent protein kinase kinase 2
Mouse - 588 5 F Camkk2 calcium/calmodulin-dependent protein kinase kinase 2, beta
Rat - 587 12q16 Camkk2 calcium/calmodulin-dependent protein kinase kinase 2
Previous and Unofficial Names
calcium/calmodulin-dependent protein kinase kinase beta | Ca+/Calmodulin-dependent protein kinase kinase beta (CaM-kinase kinase beta) | CaM-kinase kinase beta | CAMKKB | calcium/calmodulin-dependent protein kinase kinase 2, beta | calcium/calmodulin-dependent protein kinase kinase 2
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human calcium/calmodulin-dependent protein kinase kinase 2, beta, CaMKK2 kinase domain in complex with STO-609
PDB Id:  2ZV2
Ligand:  STO609
Resolution:  2.4Å
Species:  Human
References:  3
Enzyme Reaction
EC Number: 2.7.11.17

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
STO609 Hs Inhibition 7.4 pIC50 4
pIC50 7.4 (IC50 4x10-8 M) [4]
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 2,5

Key to terms and symbols Click column headers to sort
Target used in screen: CAMKK2
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 9.8 pKd
NVP-TAE684 Hs Inhibitor Inhibition 8.0 pKd
lestaurtinib Hs Inhibitor Inhibition 7.8 pKd
BI-2536 Hs Inhibitor Inhibition 7.6 pKd
PHA-665752 Hs Inhibitor Inhibition 7.1 pKd
midostaurin Hs Inhibitor Inhibition 7.1 pKd
AST-487 Hs Inhibitor Inhibition 6.7 pKd
alvocidib Hs Inhibitor Inhibition 6.4 pKd
KW-2449 Hs Inhibitor Inhibition 6.3 pKd
A-674563 Hs Inhibitor Inhibition 6.1 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: ...1

Key to terms and symbols Click column headers to sort
Target used in screen: nd/CAMKK2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 0.2
Gö 6976 Hs Inhibitor Inhibition 3.9
midostaurin Hs Inhibitor Inhibition 3.9
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 5.4
K-252a Hs Inhibitor Inhibition 6.6
SB 218078 Hs Inhibitor Inhibition 7.9
STO609 Hs Inhibitor Inhibition 7.9
JAK3 inhibitor VI Hs Inhibitor Inhibition 10.1
indirubin derivative E804 Hs Inhibitor Inhibition 26.0
SU6656 Hs Inhibitor Inhibition 27.3
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]

2. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

3. Kukimoto-Niino M, Yoshikawa S, Takagi T, Ohsawa N, Tomabechi Y, Terada T, Shirouzu M, Suzuki A, Lee S, Yamauchi T et al.. (2011) Crystal structure of the Ca²⁺/calmodulin-dependent protein kinase kinase in complex with the inhibitor STO-609. J. Biol. Chem., 286 (25): 22570-9. [PMID:21504895]

4. Tokumitsu H, Inuzuka H, Ishikawa Y, Ikeda M, Saji I, Kobayashi R. (2002) STO-609, a specific inhibitor of the Ca(2+)/calmodulin-dependent protein kinase kinase. J. Biol. Chem., 277 (18): 15813-8. [PMID:11867640]

5. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

How to cite this page

Meta subfamily: calcium/calmodulin dependent protein kinase kinase 2. Last modified on 30/03/2016. Accessed on 24/10/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1957.