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ribosomal protein S6 kinase A4

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Target not currently curated in GtoImmuPdb

Target id: 1524

Nomenclature: ribosomal protein S6 kinase A4

Abbreviated Name: MSK2

Family: MSK subfamily

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 772 11q13.1 RPS6KA4 ribosomal protein S6 kinase A4
Mouse - 773 19 A Rps6ka4 ribosomal protein S6 kinase, polypeptide 4
Rat - 773 1q43 Rps6ka4 ribosomal protein S6 kinase A4
Previous and Unofficial Names Click here for help
Ccdc88b | coiled-coil domain containing 88B | nuclear mitogen- and stress-activated protein kinase 2 | ribosomal protein kinase B | ribosomal protein S6 kinase | ribosomal protein S6 kinase, 90kDa, polypeptide 4 | Ribosomal protein S6 kinase α4 | ribosomal protein S6 kinase alpha-4 | ribosomal protein S6 kinase, polypeptide 4 | RSK-B
Database Links Click here for help
Alphafold
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 2.7.11.1

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
compound 23 [PMID: 35816678] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 pIC50 5
pIC50 7.1 (IC50 8.5x10-8 M) [5]
compound 8 [PMID: 17480064] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.5 pIC50 2
pIC50 5.5 (IC50 3.01x10-6 M) [2]
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: 3,6

Key to terms and symbols Click column headers to sort
Target used in screen: RPS6KA4(Kin.Dom.1-N-terminal)
Ligand Sp. Type Action Value Parameter
lestaurtinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 7.2 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.2 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.9 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 5.7 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 5.7 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.6 pKd
Target used in screen: RPS6KA4(Kin.Dom.2-C-terminal)
Ligand Sp. Type Action Value Parameter
BI-2536 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.4 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.5 pKd
GSK-461364A Small molecule or natural product Hs Inhibitor Inhibition 6.1 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.0 pKd
gefitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.9 pKd
lestaurtinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 5.9 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: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: MSK2/MSK2(RPS6KA4)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Small molecule or natural product Hs Inhibitor Inhibition 2.5 -1.0 0.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 0.5 -0.5
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 12.4 56.0 64.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 16.8 12.0 8.0
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 21.7 15.0 2.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 28.0 20.0 6.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 29.9 2.0 5.0
Ro-32-0432 Small molecule or natural product Hs Inhibitor Inhibition 33.3
GF109203X Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 34.9 18.0 3.0
H-89 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 38.8 9.0 2.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 2 GO processes
GO:0001818 negative regulation of cytokine production TAS
GO:0070498 interleukin-1-mediated signaling pathway IMP
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0006954 inflammatory response IEA

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. Anderson DR, Meyers MJ, Vernier WF, Mahoney MW, Kurumbail RG, Caspers N, Poda GI, Schindler JF, Reitz DB, Mourey RJ. (2007) Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J Med Chem, 50 (11): 2647-54. [PMID:17480064]

3. 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]

4. 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]

5. Ladduwahetty T, Lee MR, Maillard MC, Cachope R, Todd D, Barnes M, Beaumont V, Chauhan A, Gallati C, Haughan AF et al.. (2022) Identification of a Potent, Selective, and Brain-Penetrant Rho Kinase Inhibitor and its Activity in a Mouse Model of Huntington's Disease. J Med Chem, [Epub ahead of print]. DOI: 10.1021/acs.jmedchem.2c00474 [PMID:35816678]

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

MSK subfamily: ribosomal protein S6 kinase A4. Last modified on 13/07/2022. Accessed on 04/12/2022. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1524.