ribosomal protein S6 kinase A2 | RSK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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ribosomal protein S6 kinase A2

Target not currently curated in GtoImmuPdb

Target id: 1529

Nomenclature: ribosomal protein S6 kinase A2

Abbreviated Name: RSK3

Family: RSK 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 - 741 6q27 RPS6KA2 ribosomal protein S6 kinase A2
Mouse - 733 17 F4 Rps6ka2 ribosomal protein S6 kinase, polypeptide 2
Rat - 733 1q11 Rps6ka2 ribosomal protein S6 kinase A2
Previous and Unofficial Names
MAPKAPK1C | RSKα2 | ribosomal protein S6 kinase, 90kD, polypeptide 2 | ribosomal protein S6 kinase alpha-2 | p90rsk | HU-2 | ribosomal protein S6 kinase, 90kDa, polypeptide 2 | ribosomal protein S6 kinase polypeptide 2 | ribosomal protein S6 kinase, polypeptide 2 | ribosomal protein S6 kinase
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: 2.7.11.1

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
compound 25b [PMID: 22564207] Hs Inhibition 8.1 pIC50 4
pIC50 8.1 (IC50 7x10-9 M) [4]
BI-D1870 Hs Inhibition 7.7 pIC50 5
pIC50 7.7 (IC50 1.8x10-8 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: RSK3(Kin.Dom.1-N-terminal)
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 8.1 pKd
sunitinib Hs Inhibitor Inhibition 7.8 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.5 pKd
lestaurtinib Hs Inhibitor Inhibition 7.1 pKd
enzastaurin Hs Inhibitor Inhibition 6.7 pKd
SU-14813 Hs Inhibitor Inhibition 6.6 pKd
ruboxistaurin Hs Inhibitor Inhibition 6.6 pKd
dovitinib Hs Inhibitor Inhibition 6.5 pKd
KW-2449 Hs Inhibitor Inhibition 6.2 pKd
midostaurin Hs Inhibitor Inhibition 6.1 pKd
Target used in screen: RSK3(Kin.Dom.2-C-terminal)
Ligand Sp. Type Action Value Parameter
ruxolitinib Hs Inhibitor Inhibition 6.8 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.8 pKd
staurosporine Hs Inhibitor Inhibition 6.7 pKd
R547 Hs Inhibitor Inhibition 6.4 pKd
tofacitinib Hs Inhibitor Inhibition 6.2 pKd
BI-2536 Hs Inhibitor Inhibition 6.2 pKd
AST-487 Hs Inhibitor Inhibition 6.0 pKd
lestaurtinib Hs Inhibitor Inhibition 5.9 pKd
alvocidib Hs Inhibitor Inhibition 5.8 pKd
fedratinib Hs Inhibitor Inhibition 5.6 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: Rsk3/RSK3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Gö 6976 Hs Inhibitor Inhibition 0.3 0.0 -1.0
SB 218078 Hs Inhibitor Inhibition 1.3 8.0 8.0
GF109203X Hs Inhibitor Inhibition 1.4 1.0 -1.0
staurosporine Hs Inhibitor Inhibition 1.6 1.0 0.0
K-252a Hs Inhibitor Inhibition 1.7 0.0 1.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 2.1 0.0 -1.0
midostaurin Hs Inhibitor Inhibition 3.1 1.0 0.0
PKCbeta inhibitor Hs Inhibitor Inhibition 3.2 0.0 -1.0
Ro-32-0432 Hs Inhibitor Inhibition 3.6
Gö 6983 Hs Inhibitor Inhibition 5.5 0.0 -2.0
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. Gingrich DE, Lisko JG, Curry MA, Cheng M, Quail M, Lu L, Wan W, Albom MS, Angeles TS, Aimone LD et al.. (2012) Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase. J. Med. Chem., 55 (10): 4580-93. [PMID:22564207]

5. Sapkota GP, Cummings L, Newell FS, Armstrong C, Bain J, Frodin M, Grauert M, Hoffmann M, Schnapp G, Steegmaier M et al.. (2007) BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem. J., 401 (1): 29-38. [PMID:17040210]

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

RSK subfamily: ribosomal protein S6 kinase A2. Last modified on 30/03/2016. Accessed on 20/08/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1529.