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Casein kinase 2

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Target id: 1548

Nomenclature: Casein kinase 2

Abbreviated Name: CK2

Family: Casein kinase 2 (CK2) family

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BRENDA
KEGG Enzyme
Enzyme Reaction Click here for help
EC Number: 2.7.11.1

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
DMAT Small molecule or natural product Primary target of this compound Ligand has a PDB structure Immunopharmacology Ligand Rn Inhibition 7.4 pKi
pKi 7.4 (Ki 4x10-8 M)
TBBt Small molecule or natural product Ligand has a PDB structure Rn Inhibition 6.4 pKi 7
pKi 6.4 (Ki 4x10-7 M) [7]
CX-5279 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.0 pIC50 1
pIC50 9.0 (IC50 9.1x10-10 M) [1]
Description: Recombinant human CK2 holoenzyme containiny wild-type alpha subunits.
CX-5011 Small molecule or natural product Rn Inhibition 9.0 pIC50 1
pIC50 9.0 (IC50 9.7x10-10 M) [1]
Description: Native rat CK2 isolated from liver.
CX-5011 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.6 pIC50 1
pIC50 8.6 (IC50 2.3x10-9 M) [1]
Description: Recombinant holoenzyme with wild-type alpha subunits.
CX-5279 Small molecule or natural product Rn Inhibition 8.6 pIC50 1
pIC50 8.6 (IC50 2.73x10-9 M) [1]
Description: Native CK2 isolated from rat liver
compound 5b [PMID: 24900464] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.3 pIC50 3
pIC50 8.3 (IC50 5x10-9 M) [3]
compound 2 [PMID: 22560567] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 – 7.7 pIC50 2,4
pIC50 7.6 – 7.7 (IC50 2.7x10-8 – 1.9x10-8 M) [2,4]
casein kinase II inhibitor III Small molecule or natural product Primary target of this compound Hs Inhibition 7.0 pIC50 6
pIC50 7.0 (IC50 1.1x10-7 M) [6]
XL413 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.7 pIC50 4
pIC50 6.7 (IC50 2.15x10-7 M) [4]
DRB Small molecule or natural product Ligand has a PDB structure Hs Inhibition - - 9
[9]
View species-specific inhibitor tables
Inhibitor Comments
DMAT inhibits CK2 kinase activity in vitro (purified and endogenous enzyme assays), and promotes Jurkat cell apoptosis [5].
Immunopharmacology Comments
Protein kinase CK2 inhibition prevents TH17 cell development, driving the TH17/Treg balance towards Treg generation, an action which may find clinical utility in treating TH17-driven autoimmune diseases [8].
General Comments
Casein kinase 2 (CK2) is a heterotetrameric protein kinase, made up of 2 β subunits with two other subunits of α and/or α' composition. CK2 is the kinase that activates the transcriptional regulator BRD4.

References

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1. Battistutta R, Cozza G, Pierre F, Papinutto E, Lolli G, Sarno S, O'Brien SE, Siddiqui-Jain A, Haddach M, Anderes K et al.. (2011) Unprecedented selectivity and structural determinants of a new class of protein kinase CK2 inhibitors in clinical trials for the treatment of cancer. Biochemistry, 50 (39): 8478-88. [PMID:21870818]

2. Coffman K, Brodney M, Cook J, Lanyon L, Pandit J, Sakya S, Schachter J, Tseng-Lovering E, Wessel M. (2011) 6-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3β inhibitors. Bioorg Med Chem Lett, 21 (5): 1429-33. [PMID:21295469]

3. Dowling JE, Chuaqui C, Pontz TW, Lyne PD, Larsen NA, Block MH, Chen H, Su N, Wu A, Russell D et al.. (2012) Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization. ACS Med Chem Lett, 3 (4): 278-83. [PMID:24900464]

4. Koltun ES, Tsuhako AL, Brown DS, Aay N, Arcalas A, Chan V, Du H, Engst S, Ferguson K, Franzini M et al.. (2012) Discovery of XL413, a potent and selective CDC7 inhibitor. Bioorg Med Chem Lett, 22 (11): 3727-31. [PMID:22560567]

5. Pagano MA, Meggio F, Ruzzene M, Andrzejewska M, Kazimierczuk Z, Pinna LA. (2004) 2-Dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole: a novel powerful and selective inhibitor of protein kinase CK2. Biochem Biophys Res Commun, 321 (4): 1040-4. [PMID:15358133]

6. Pagano MA, Poletto G, Di Maira G, Cozza G, Ruzzene M, Sarno S, Bain J, Elliott M, Moro S, Zagotto G et al.. (2007) Tetrabromocinnamic acid (TBCA) and related compounds represent a new class of specific protein kinase CK2 inhibitors. Chembiochem, 8 (1): 129-39. [PMID:17133643]

7. Sarno S, de Moliner E, Ruzzene M, Pagano MA, Battistutta R, Bain J, Fabbro D, Schoepfer J, Elliott M, Furet P et al.. (2003) Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA). Biochem J, 374 (Pt 3): 639-46. [PMID:12816539]

8. Ulges A, Witsch EJ, Pramanik G, Klein M, Birkner K, Bühler U, Wasser B, Luessi F, Stergiou N, Dietzen S et al.. (2016) Protein kinase CK2 governs the molecular decision between encephalitogenic TH17 cell and Treg cell development. Proc Natl Acad Sci USA, 113 (36): 10145-50. [PMID:27555590]

9. Zandomeni R, Zandomeni MC, Shugar D, Weinmann R. (1986) Casein kinase type II is involved in the inhibition by 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole of specific RNA polymerase II transcription. J Biol Chem, 261 (7): 3414-9. [PMID:3456346]

How to cite this page

Casein kinase 2 (CK2) family: Casein kinase 2. Last modified on 05/10/2017. Accessed on 04/12/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1548.