SGK2, serine/threonine kinase 2

Target id: 1535

Nomenclature: SGK2, serine/threonine kinase 2

Abbreviated Name: SGK2

Family: SGK family

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 SGK2, serine/threonine kinase 2 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 427 20q13.2 SGK2 SGK2, serine/threonine kinase 2
Mouse - 367 2 H3 Sgk2 serum/glucocorticoid regulated kinase 2
Rat - 367 3q42 Sgk2 SGK2, serine/threonine kinase 2
Previous and Unofficial Names
serine/threonine-protein kinase Sgk2
Database Links
BRENDA
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
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
GSK650394 Hs Inhibition 7.0 pIC50 4
pIC50 7.0 (IC50 1.03x10-7 M) [4]
compound 14n [PMID: 25589934] Hs Inhibition 6.9 pIC50 3
pIC50 6.9 (IC50 1.28x10-7 M) [3]
Description: at high (500μM) ATP concentration
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: 1-2

Key to terms and symbols Click column headers to sort
Target used in screen: SGK2/SGK2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 7.8 13.5 3.0
K-252a Hs Inhibitor Inhibition 9.7 7.0 1.0
SB 218078 Hs Inhibitor Inhibition 18.6 77.0 61.0
PKR inhibitor Hs Inhibitor Inhibition 25.0 12.0 5.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 28.1 12.0 2.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 42.0 36.0 6.0
casein kinase II inhibitor III Hs Inhibitor Inhibition 59.7 83.0 41.0
SU11652 Hs Inhibitor Inhibition 62.8 60.0 32.0
Cdk4 inhibitor Hs Inhibitor Inhibition 68.5 64.0 69.0
SU9516 Hs Inhibitor Inhibition 71.4 94.0 32.0
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. 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]

3. Halland N, Schmidt F, Weiss T, Saas J, Li Z, Czech J, Dreyer M, Hofmeister A, Mertsch K, Dietz U et al.. (2015) Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors. ACS Med Chem Lett6 (1): 73-8. [PMID:25589934]

4. Sherk AB, Frigo DE, Schnackenberg CG, Bray JD, Laping NJ, Trizna W, Hammond M, Patterson JR, Thompson SK, Kazmin D et al.. (2008) Development of a small-molecule serum- and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic. Cancer Res.68 (18): 7475-83. [PMID:18794135]

How to cite this page

SGK family: SGK2, serine/threonine kinase 2. Last modified on 19/01/2017. Accessed on 21/11/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1535.