mitogen-activated protein kinase kinase kinase 2 | STE11 family | IUPHAR/BPS Guide to PHARMACOLOGY

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mitogen-activated protein kinase kinase kinase 2

Target not currently curated in GtoImmuPdb

Target id: 2077

Nomenclature: mitogen-activated protein kinase kinase kinase 2

Abbreviated Name: MEKK2

Family: STE11 family

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 - 619 2q21.1 MAP3K2 mitogen-activated protein kinase kinase kinase 2
Mouse - 619 18 B3 Map3k2 mitogen-activated protein kinase kinase kinase 2
Rat - 619 18 p12 Map3k2 mitogen activated protein kinase kinase kinase 2
Previous and Unofficial Names
MAP/ERK kinase kinase 2 | MAPKKK2 | MEK kinase 2
Database Links
BRENDA
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 the complex of human mitogen activated protein kinase kinase 5 phox domain (MAP2K5-phox) with human mitogen activated protein kinase kinase kinase 2 phox domain (MAP3K2-phox)
PDB Id:  2NPT
Resolution:  1.75Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.11.25

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 Affinity Parameter Reference
URMC-099 Hs Inhibition 6.2 pIC50 3
pIC50 6.2 (IC50 6.61x10-7 M) [3]
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: 2,4

Key to terms and symbols Click column headers to sort
Target used in screen: MAP3K2
Ligand Sp. Type Action Affinity Parameter
staurosporine Hs Inhibitor Inhibition 8.6 pKd
lestaurtinib Hs Inhibitor Inhibition 8.3 pKd
bosutinib Hs Inhibitor Inhibition 7.5 pKd
ruxolitinib Hs Inhibitor Inhibition 7.4 pKd
sunitinib Hs Inhibitor Inhibition 7.2 pKd
dovitinib Hs Inhibitor Inhibition 7.2 pKd
crizotinib Hs Inhibitor Inhibition 7.1 pKd
KW-2449 Hs Inhibitor Inhibition 7.1 pKd
SU-14813 Hs Inhibitor Inhibition 7.1 pKd
JNJ-28312141 Hs Inhibitor Inhibition 7.1 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/MEKK2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Cdk1/2 inhibitor III Hs Inhibitor Inhibition -0.5
staurosporine Hs Inhibitor Inhibition 1.2
K-252a Hs Inhibitor Inhibition 2.9
Gö 6976 Hs Inhibitor Inhibition 3.0
JNJ-7706621 Hs Inhibitor Inhibition 11.3
SB 218078 Hs Inhibitor Inhibition 14.0
SU11652 Hs Inhibitor Inhibition 20.1
bosutinib Hs Inhibitor Inhibition 23.5
Cdk2 inhibitor IV Hs Inhibitor Inhibition 25.3
midostaurin Hs Inhibitor Inhibition 30.2
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. Goodfellow VS, Loweth CJ, Ravula SB, Wiemann T, Nguyen T, Xu Y, Todd DE, Sheppard D, Pollack S, Polesskaya O et al.. (2013) Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. J. Med. Chem., 56 (20): 8032-48. [PMID:24044867]

4. 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

STE11 family: mitogen-activated protein kinase kinase kinase 2. Last modified on 18/02/2015. Accessed on 20/02/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2077.