mitogen-activated protein kinase 8

Nomenclature: mitogen-activated protein kinase 8

Abbreviated Name: JNK1

Family: JNK 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 - 384 10q11 MAPK8 mitogen-activated protein kinase 8
Mouse - 384 14 B Mapk8 mitogen-activated protein kinase 8
Rat - 427 16p16 Mapk8 mitogen-activated protein kinase 8
Previous and Unofficial Names
c-Jun N-terminal kinase
JUN N-terminal kinase
JNK
SAPK1
SAPK1C
MAP kinase 8
MAPK 8
SAPK gamma
c-Jun N-terminal kinase 1
c-jun NH2-terminal kinase
p54 gamma
stress-activated protein kinase JNK1
Prkm8
PRKM8
JNK-46
Stress-activated protein kinase 1c
Jnk1
Database Links
BRENDA
Ensembl Gene
Entrez Gene
ExplorEnz
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG BRITE Hierarchy
KEGG Gene
OMIM
PhosphoSitePlus
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Jnk1 complexed with a bis-anilino-pyrrolopyrimidine inhibitor.
PDB Id:  3ELJ
Resolution:  1.8Å
Species:  Human
References:  3
Enzyme Reaction
EC Number: 2.7.11.24
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
SP600125 Hs Inhibition 7.4 pIC50 2
pIC50 7.4 (IC50 4x10-8 M) [2]
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: 4,6

Key to terms and symbols Click column headers to sort
Target used in screen: JNK1
Ligand Sp. Type Action Affinity Units
lestaurtinib Hs Inhibitor Inhibition 7.96 pKd
R406 Hs Inhibitor Inhibition 7.42 pKd
TAE 684 Hs Inhibitor Inhibition 6.8 pKd
GSK-1838705A Hs Inhibitor Inhibition 6.68 pKd
staurosporine Hs Inhibitor Inhibition 6.66 pKd
TG-101348 Hs Inhibitor Inhibition 6.59 pKd
nilotinib Hs Inhibitor Inhibition 6.35 pKd
AST-487 Hs Inhibitor Inhibition 6.34 pKd
KW-2449 Hs Inhibitor Inhibition 6.24 pKd
JNJ-28312141 Hs Inhibitor Inhibition 6.08 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: 1,5

Key to terms and symbols Click column headers to sort
Target used in screen: JNK1α1/JNK1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
JNK inhibitor VIII Hs Inhibitor Inhibition 28.1 -16.0 -6.0
K-252a Hs Inhibitor Inhibition 28.8 -12.0 -20.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 51.1 44.0 -11.0
PD 174265 Hs Inhibitor Inhibition 73.7 94.0 76.0
JAK inhibitor I Hs Inhibitor Inhibition 73.7 32.0 9.0
aloisine Hs Inhibitor Inhibition 74.5 105.0 103.0
BAY 11-7082 Hs Inhibitor Inhibition 74.7 115.0 96.0
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 78.3 114.0 83.0
Gö 6976 Hs Inhibitor Inhibition 78.7 88.0 31.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 78.8 88.0 84.0
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. Bennett BL, Sasaki DT, Murray BW, O'Leary EC, Sakata ST, Xu W, Leisten JC, Motiwala A, Pierce S, Satoh Y et al.. (2001) SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proc. Natl. Acad. Sci. U.S.A.98 (24): 13681-6. [PMID:11717429]

3. Chamberlain SD, Redman AM, Wilson JW, Deanda F, Shotwell JB, Gerding R, Lei H, Yang B, Stevens KL, Hassell AM et al.. (2009) Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity. Bioorg. Med. Chem. Lett.19 (2): 360-4. [PMID:19071018]

4. 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]

5. 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]

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

JNK subfamily: mitogen-activated protein kinase 8. Last modified on 17/09/2013. Accessed on 02/10/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1496.