mitogen-activated protein kinase kinase kinase 8 | STE-unique family | IUPHAR/BPS Guide to PHARMACOLOGY

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mitogen-activated protein kinase kinase kinase 8

Target not currently curated in GtoImmuPdb

Target id: 2083

Nomenclature: mitogen-activated protein kinase kinase kinase 8

Abbreviated Name: Cot

Family: STE-unique 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 - 467 10p11.2 MAP3K8 mitogen-activated protein kinase kinase kinase 8
Mouse - 467 18 A1 Map3k8 mitogen-activated protein kinase kinase kinase 8
Rat - 467 17 q12.1 Map3k8 mitogen-activated protein kinase kinase kinase 8
Previous and Unofficial Names
Cancer Osaka thyroid oncogene | ESTF | proto-oncogene c-COT | serine/threonine kinase (Tpl-2)
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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 Value Parameter Reference
MEK inhibitor II Hs Inhibition 7.3 pIC50 2
pIC50 7.3 (IC50 5x10-8 M) [2]
Tpl2 kinase inhibitor Hs Inhibition 7.3 pIC50 3
pIC50 7.3 (IC50 5x10-8 M) [3]
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/COT1(MAP3K8)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Src kinase inhibitor I Hs Inhibitor Inhibition 68.9
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 75.9
Tpl2 kinase inhibitor Hs Inhibitor Inhibition 79.1
MEK inhibitor I Hs Inhibitor Inhibition 79.8
Cdk1/5 inhibitor Hs Inhibitor Inhibition 81.3
SU11274 Hs Inhibitor Inhibition 82.9
casein kinase II inhibitor III Hs Inhibitor Inhibition 83.0
Lck inhibitor Hs Inhibitor Inhibition 83.3
fascaplysin Hs Inhibitor Inhibition 84.9
PD98059 Hs Inhibitor Inhibition 85.7
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. Fedorov O, Marsden B, Pogacic V, Rellos P, Müller S, Bullock AN, Schwaller J, Sundström M, Knapp S. (2007) A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc. Natl. Acad. Sci. U.S.A., 104 (51): 20523-8. [PMID:18077363]

3. Gavrin LK, Green N, Hu Y, Janz K, Kaila N, Li HQ, Tam SY, Thomason JR, Gopalsamy A, Ciszewski G et al.. (2005) Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships. Bioorg. Med. Chem. Lett., 15 (23): 5288-92. [PMID:16165349]

How to cite this page

STE-unique family: mitogen-activated protein kinase kinase kinase 8. Last modified on 23/10/2014. Accessed on 18/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2083.