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serum/glucocorticoid regulated kinase 2

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Target not currently curated in GtoImmuPdb

Target id: 1535

Nomenclature: serum/glucocorticoid regulated kinase 2

Abbreviated Name: SGK2

Family: SGK family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 427 20q13.12 SGK2 serum/glucocorticoid regulated kinase 2
Mouse - 367 2 H2 Sgk2 serum/glucocorticoid regulated kinase 2
Rat - 367 3q42 Sgk2 serum/glucocorticoid regulated kinase 2
Previous and Unofficial Names Click here for help
serine/threonine-protein kinase Sgk2 | SGK2 | SGK2, serine/threonine kinase 2
Database Links Click here for help
Alphafold Q9HBY8 (Hs), Q9QZS5 (Mm), Q8R4U9 (Rn)
BRENDA 2.7.11.1
ChEMBL Target CHEMBL5794 (Hs)
Ensembl Gene ENSG00000101049 (Hs), ENSMUSG00000017868 (Mm), ENSRNOG00000033573 (Rn)
Entrez Gene 10110 (Hs), 27219 (Mm), 171497 (Rn)
Human Protein Atlas ENSG00000101049 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:10110 (Hs), mmu:27219 (Mm), rno:171497 (Rn)
OMIM 607589 (Hs)
Pharos Q9HBY8 (Hs)
RefSeq Nucleotide NM_001199264 (Hs), NM_013731 (Mm), NM_134463 (Rn)
RefSeq Protein NP_057360 (Hs), NP_038759 (Mm), NP_604458 (Rn)
UniProtKB Q9HBY8 (Hs), Q9QZS5 (Mm), Q8R4U9 (Rn)
Wikipedia SGK2 (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

Activators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
privosegtor Small molecule or natural product Hs Activation - - 5
⤷ [5]
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
GSK650394 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.0 pIC50 4
⤷ pIC50 7.0 (IC50 1.03x10-7 M) [4]
compound 14n [PMID: 25589934] Small molecule or natural product Click here for species-specific activity table 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 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: 1-2
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 13.5 3.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 9.7 7.0 1.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 18.6 77.0 61.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 25.0 12.0 5.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 28.1 12.0 2.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 42.0 36.0 6.0
casein kinase II inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 59.7 83.0 41.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 62.8 60.0 32.0
Cdk4 inhibitor Small molecule or natural product Hs Inhibitor Inhibition 68.5 64.0 69.0
SU9516 Small molecule or natural product Ligand has a PDB structure 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 Lett, 6 (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]

5. Villoslada P, Vila G, Colafrancesco V, Moreno B, Fernandez-Diez B, Vazquez R, Pertsovskaya I, Zubizarreta I, Pulido-Valdeolivas I, Messeguer J et al.. (2019) Axonal and Myelin Neuroprotection by the Peptoid BN201 in Brain Inflammation. Neurotherapeutics, 16 (3): 808-827. [PMID:30815844]

How to cite this page

SGK family: serum/glucocorticoid regulated kinase 2. Last modified on 11/03/2024. Accessed on 20/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1535.