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calcium/calmodulin dependent protein kinase kinase 2

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Target not currently curated in GtoImmuPdb

Target id: 1957

Nomenclature: calcium/calmodulin dependent protein kinase kinase 2

Abbreviated Name: CAMKK2

Family: Meta subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 588 12q24.31 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 Click here for help
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 Click here for help
Alphafold Q96RR4 (Hs), Q8C078 (Mm), O88831 (Rn)
BRENDA 2.7.11.17
ChEMBL Target CHEMBL5284 (Hs), CHEMBL4295888 (Mm), CHEMBL1795115 (Rn)
Ensembl Gene ENSG00000110931 (Hs), ENSMUSG00000029471 (Mm), ENSRNOG00000001309 (Rn)
Entrez Gene 10645 (Hs), 207565 (Mm), 83506 (Rn)
Human Protein Atlas ENSG00000110931 (Hs)
KEGG Enzyme 2.7.11.17
KEGG Gene hsa:10645 (Hs), mmu:207565 (Mm), rno:83506 (Rn)
OMIM 615002 (Hs)
Pharos Q96RR4 (Hs)
RefSeq Nucleotide NM_001270485 (Hs), NM_001199676 (Mm), NM_031338 (Rn)
RefSeq Protein NP_006540 (Hs), NP_001186605 (Mm), NP_112628 (Rn)
UniProtKB Q96RR4 (Hs), Q8C078 (Mm), O88831 (Rn)
Wikipedia CAMKK2 (Hs)
Selected 3D Structures Click here for help
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 Click here for help
EC Number: 2.7.11.17

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
STO609 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.4 pIC50 4
⤷ pIC50 7.4 (IC50 4x10-8 M) [4]
DiscoveRx KINOMEscan® screen Click here for help
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.8 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.8 pKd
BI-2536 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.1 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 7.1 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.3 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure 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 Click here for help
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 0.2
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 3.9
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 3.9
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.4
K-252a Small molecule or natural product Hs Inhibitor Inhibition 6.6
STO609 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.9
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 7.9
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 10.1
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 26.0
SU6656 Small molecule or natural product Ligand has a PDB structure 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 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1957.