ribosomal protein S6 kinase A6 | RSK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

ribosomal protein S6 kinase A6

Target id: 1530

Nomenclature: ribosomal protein S6 kinase A6

Abbreviated Name: RSK4

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

   GtoImmuPdb view: OFF :     Currently no data for ribosomal protein S6 kinase A6 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 745 Xq21.1 RPS6KA6 ribosomal protein S6 kinase A6
Mouse - 860 X Rps6ka6 ribosomal protein S6 kinase polypeptide 6
Rat - 860 Xq31 Rps6ka6 ribosomal protein S6 kinase A6
Previous and Unofficial Names
RSKα6 | ribosomal protein S6 kinase, 90kD, polypeptide 6 | ribosomal protein S6 kinase alpha-6 | ribosomal protein S6 kinase, 90kDa, polypeptide 6
Database Links
BRENDA
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 Affinity Units Reference
BI-D1870 Hs Inhibition 7.8 pIC50 6
pIC50 7.8 (IC50 1.5x10-8 M) [6]
AT-9283 Hs Inhibition 7.5 – 8.0 pIC50 5
pIC50 7.5 – 8.0 (IC50 3x10-8 – 1x10-8 M) [5]
compound 25b [PMID: 22564207] Hs Inhibition 7.7 pIC50 4
pIC50 7.7 (IC50 1.9x10-8 M) [4]
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: 2,7

Key to terms and symbols Click column headers to sort
Target used in screen: RSK4(Kin.Dom.1-N-terminal)
Ligand Sp. Type Action Affinity Units
staurosporine Hs Inhibitor Inhibition 7.7 pKd
enzastaurin Hs Inhibitor Inhibition 7.6 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.6 pKd
lestaurtinib Hs Inhibitor Inhibition 7.0 pKd
GSK-461364A Hs Inhibitor Inhibition 6.5 pKd
KW-2449 Hs Inhibitor Inhibition 6.4 pKd
PP-242 Hs Inhibitor Inhibition 6.2 pKd
ruxolitinib Hs Inhibitor Inhibition 5.8 pKd
midostaurin Hs Inhibitor Inhibition 5.8 pKd
alvocidib Hs Inhibitor Inhibition 5.7 pKd
Target used in screen: RSK4(Kin.Dom.2-C-terminal)
Ligand Sp. Type Action Affinity Units
ruxolitinib Hs Inhibitor Inhibition 6.8 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.8 pKd
vandetanib Hs Inhibitor Inhibition 6.6 pKd
SB203580 Hs Inhibitor Inhibition 6.6 pKd
fedratinib Hs Inhibitor Inhibition 6.4 pKd
tofacitinib Hs Inhibitor Inhibition 6.3 pKd
alvocidib Hs Inhibitor Inhibition 6.1 pKd
TG-100-115 Hs Inhibitor Inhibition 6.0 pKd
BI-2536 Hs Inhibitor Inhibition 5.9 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 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: Rsk4/RSK4
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
SB 218078 Hs Inhibitor Inhibition 1.1 9.0 17.0
midostaurin Hs Inhibitor Inhibition 1.2 0.0 3.0
K-252a Hs Inhibitor Inhibition 1.7 -2.0 3.0
staurosporine Hs Inhibitor Inhibition 1.7 2.0 1.0
PKCbeta inhibitor Hs Inhibitor Inhibition 2.0 5.0 2.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 2.4 -2.0 -2.0
Ro-32-0432 Hs Inhibitor Inhibition 2.9
GF109203X Hs Inhibitor Inhibition 4.0 4.0 3.0
Gö 6976 Hs Inhibitor Inhibition 4.2 4.0 4.0
Gö 6983 Hs Inhibitor Inhibition 4.5 4.0 2.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

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. Howard S, Berdini V, Boulstridge JA, Carr MG, Cross DM, Curry J, Devine LA, Early TR, Fazal L, Gill AL et al.. (2009) Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity. J. Med. Chem., 52 (2): 379-88. [PMID:19143567]

6. 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]

7. 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 A6. Last modified on 30/03/2016. Accessed on 17/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1530.