SIK family kinase 3 | QIK subfamily | IUPHAR/BPS Guide to PHARMACOLOGY

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SIK family kinase 3

target has curated data in GtoImmuPdb

Target id: 2199

Nomenclature: SIK family kinase 3

Abbreviated Name: QSK

Family: QIK 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 - 1263 11q23.3 SIK3 SIK family kinase 3
Mouse - 1369 9 A5.2 Sik3 SIK family kinase 3
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
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
ARN-3236 Hs Inhibition 8.2 pIC50 4
pIC50 8.2 (IC50 6.6x10-9 M) [4]
Description: In an in vitro enzymatic assay.
HG-9-91-01 Hs Inhibition 8.0 pIC50 1
pIC50 8.0 (IC50 9.6x10-9 M) [1]
dasatinib Hs Inhibition 8.0 pIC50 5
pIC50 8.0 (IC50 1x10-8 M) [5]
bosutinib 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: 3,6

Key to terms and symbols Click column headers to sort
Target used in screen: QSK
Ligand Sp. Type Action Value Parameter
staurosporine Hs Inhibitor Inhibition 9.3 pKd
dasatinib Hs Inhibitor Inhibition 7.6 pKd
bosutinib Hs Inhibitor Inhibition 7.2 pKd
midostaurin Hs Inhibitor Inhibition 7.0 pKd
PD-173955 Hs Inhibitor Inhibition 7.0 pKd
lestaurtinib Hs Inhibitor Inhibition 6.9 pKd
canertinib Hs Inhibitor Inhibition 6.2 pKd
NVP-TAE684 Hs Inhibitor Inhibition 5.9 pKd
ruxolitinib Hs Inhibitor Inhibition 5.9 pKd
fedratinib Hs Inhibitor Inhibition 5.7 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
Inhibition of SIK2 and SIK3 to promote macrophage switch to a 'regulatory'-like phenotype that favours resolution of inflammation is considered a potential therapeutic strategy for the treatment of chronic inflammatory diseases [2,5].

References

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1. Clark K, MacKenzie KF, Petkevicius K, Kristariyanto Y, Zhang J, Choi HG, Peggie M, Plater L, Pedrioli PG, McIver E et al.. (2012) Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc. Natl. Acad. Sci. U.S.A., 109 (42): 16986-91. [PMID:23033494]

2. Darling NJ, Toth R, Arthur JS, Clark K. (2017) Inhibition of SIK2 and SIK3 during differentiation enhances the anti-inflammatory phenotype of macrophages. Biochem. J., 474 (4): 521-537. [PMID:27920213]

3. 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]

4. Lombardi MS, Gilliéron C, Dietrich D, Gabay C. (2016) SIK inhibition in human myeloid cells modulates TLR and IL-1R signaling and induces an anti-inflammatory phenotype. J. Leukoc. Biol., 99 (5): 711-21. [PMID:26590148]

5. Ozanne J, Prescott AR, Clark K. (2015) The clinically approved drugs dasatinib and bosutinib induce anti-inflammatory macrophages by inhibiting the salt-inducible kinases. Biochem. J., 465 (2): 271-9. [PMID:25351958]

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

QIK subfamily: SIK family kinase 3. Last modified on 23/05/2017. Accessed on 07/04/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2199.