mitogen-activated protein kinase kinase 6 | STE7 family | IUPHAR/BPS Guide to PHARMACOLOGY

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mitogen-activated protein kinase kinase 6

Target not currently curated in GtoImmuPdb

Target id: 2067

Nomenclature: mitogen-activated protein kinase kinase 6

Abbreviated Name: MKK6

Family: STE7 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 - 334 17q MAP2K6 mitogen-activated protein kinase kinase 6
Mouse - 334 11 E1 Map2k6 mitogen-activated protein kinase kinase 6
Rat - 334 10 q32.1 Map2k6 mitogen-activated protein kinase kinase 6
Previous and Unofficial Names
dual specificity mitogen-activated protein kinase kinase 6 | MAP kinase kinase 6 | MEK6 | PRKMK6 | SAPK kinase 3 | SAPKK3 | SKK3 | Stress-activated protein kinase kinase 3
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Refined Crystal structure of non-phosphorylated MAP2K6 in a putative auto-inhibition state
PDB Id:  3VN9
Resolution:  2.6Å
Species:  Human
References:  4
Enzyme Reaction
EC Number: 2.7.12.2

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
staurosporine Hs Inhibition >9.0 pIC50 5
pIC50 >9.0 (IC50 <1x10-9 M) [5]
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: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: MEK6
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 8.5 pKd
lestaurtinib Hs Inhibitor Inhibition 7.4 pKd
tamatinib Hs Inhibitor Inhibition 6.3 pKd
KW-2449 Hs Inhibitor Inhibition 6.1 pKd
bosutinib Hs Inhibitor Inhibition 5.9 pKd
NVP-TAE684 Hs Inhibitor Inhibition 5.7 pKd
tozasertib Hs Inhibitor Inhibition 5.6 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
crizotinib Hs Inhibitor Inhibition <5.5 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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: MKK6/MKK6
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 9.6 26.0 0.0
staurosporine Hs Inhibitor Inhibition 15.2 1.0 -1.5
SB 218078 Hs Inhibitor Inhibition 19.3 27.0 10.0
Gö 6976 Hs Inhibitor Inhibition 21.1 0.0 1.0
PKR inhibitor Hs Inhibitor Inhibition 56.8 -1.0 1.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 62.7 26.0 20.0
isogranulatimide Hs Inhibitor Inhibition 65.7 69.0 21.0
sunitinib Hs Inhibitor Inhibition 75.9
JAK3 inhibitor VI Hs Inhibitor Inhibition 78.8 22.0 3.0
p38 MAP kinase inhibitor Hs Inhibitor Inhibition 79.4 74.0 0.0
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. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

4. Matsumoto T, Kinoshita T, Matsuzaka H, Nakai R, Kirii Y, Yokota K, Tada T. (2012) Crystal structure of non-phosphorylated MAP2K6 in a putative auto-inhibition state. J. Biochem., 151 (5): 541-9. [PMID:22383536]

5. Pandey A, Volkots DL, Seroogy JM, Rose JW, Yu JC, Lambing JL, Hutchaleelaha A, Hollenbach SJ, Abe K, Giese NA et al.. (2002) Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family. J. Med. Chem., 45 (17): 3772-93. [PMID:12166950]

6. 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

STE7 family: mitogen-activated protein kinase kinase 6. Last modified on 12/02/2015. Accessed on 19/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2067.