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ribosomal protein S6 kinase A2

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Target not currently curated in GtoImmuPdb

Target id: 1529

Nomenclature: ribosomal protein S6 kinase A2

Abbreviated Name: RSK3

Family: RSK subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 733 6q27 RPS6KA2 ribosomal protein S6 kinase A2
Mouse - 733 17 4.7 cM Rps6ka2 ribosomal protein S6 kinase, polypeptide 2
Rat - 733 1q11 Rps6ka2 ribosomal protein S6 kinase A2
Previous and Unofficial Names Click here for help
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 Click here for help
Alphafold Q15349 (Hs), Q9WUT3 (Mm)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL3906 (Hs), CHEMBL3351220 (Mm)
Ensembl Gene ENSG00000071242 (Hs), ENSMUSG00000023809 (Mm), ENSRNOG00000013194 (Rn)
Entrez Gene 6196 (Hs), 20112 (Mm), 117269 (Rn)
Human Protein Atlas ENSG00000071242 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:6196 (Hs), mmu:20112 (Mm), rno:117269 (Rn)
OMIM 601685 (Hs)
Pharos Q15349 (Hs)
RefSeq Nucleotide NM_001006932 (Hs), NM_011299 (Mm), NM_057128 (Rn)
RefSeq Protein NP_001006933 (Hs), NP_035429 (Mm), NP_476469 (Rn)
UniProtKB Q15349 (Hs), Q9WUT3 (Mm)
Wikipedia RPS6KA2 (Hs)
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 25b [PMID: 22564207] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 4
⤷ pIC50 8.1 (IC50 7x10-9 M) [4]
BI-D1870 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.7 pIC50 5
⤷ pIC50 7.7 (IC50 1.8x10-8 M) [5]
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: 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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.1 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.5 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.1 pKd
enzastaurin Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.6 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.5 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.2 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.1 pKd
Target used in screen: RSK3(Kin.Dom.2-C-terminal)
Ligand Sp. Type Action Value Parameter
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.8 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
R547 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
tofacitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.2 pKd
BI-2536 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 6.0 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.9 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure 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 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: 1,3
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 0.3 0.0 -1.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 1.3 8.0 8.0
GF109203X Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.4 1.0 -1.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.6 1.0 0.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 1.7 0.0 1.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.1 0.0 -1.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 3.1 1.0 0.0
PKCbeta inhibitor Small molecule or natural product Hs Inhibitor Inhibition 3.2 0.0 -1.0
Ro-32-0432 Small molecule or natural product Hs Inhibitor Inhibition 3.6
Gö 6983 Small molecule or natural product 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 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1529.