CK2
CK2 (casein kinase 2) is a conserved, constitutively active serine/threonine kinase that regulates protein stability, protein-protein interactions, and subcellular localization through phosphorylation[1]. Mechanistically, CK2 connects developmental and cancer biology through Wnt and NF-κB signaling, and loss of catalytic subunits can be lethal in development[1]. In cancer contexts, CK2 supports malignant phenotypes by influencing apoptosis, DNA damage responses, and cell-cycle regulation[2]. Compared with related catalytic isoforms, CK2α′ shows distinct disease relevance because TNF-induced CK2α′ phosphorylates BRMS1 at Ser30, promoting 14-3-3ε-mediated nuclear export and proteasomal degradation in NSCLC metastasis models[3]. In orthotopic lung cancer metastasis models, BRMS1 Ser30 mutation or CX-4945 reduced CK2α′-induced migration, invasion, and metastasis[3]. CK2 also regulates immune differentiation because CX-4945 inhibited Th17 differentiation, promoted Foxp3+ Treg generation, and suppressed PI3K/Akt/mTOR activation and STAT3 phosphorylation[4]. For experimental applications, CK2 inhibitors such as CX-4945 provide tools to test CK2-dependent signaling, tumor invasion, metastasis, and immune-cell polarization[3][4][5].
References:
- [1]. Dominguez I, et al. Protein kinase CK2 in health and disease: CK2 and its role in Wnt and NF-kappaB signaling: linking development and cancer. Cell Mol Life Sci. 2009 Jun;66(11-12):1850-7. [Content Brief]
- [2]. Borgo C, et al. Protein kinase CK2: a potential therapeutic target for diverse human diseases. Signal Transduct Target Ther. 2021 May 17;6(1):183. [Content Brief]
- [3]. Liu Y, et al. CK2α' Drives Lung Cancer Metastasis by Targeting BRMS1 Nuclear Export and Degradation. Cancer Res. 2016 May 1;76(9):2675-86. [Content Brief]
- [4]. Gibson SA, et al. Protein Kinase CK2 Controls the Fate between Th17 Cell and Regulatory T Cell Differentiation. J Immunol. 2017 Jun 1;198(11):4244-4254. [Content Brief]
- [5]. Cozza G, et al. How druggable is protein kinase CK2? Med Res Rev. 2010 May;30(3):419-62. [Content Brief]
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CK2 Related Products (54)
Related Products (54)
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Antibodies (1)
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Emodin
0 ImagesEmodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice.
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CK2-IN-17
0 ImagesCat. No.: HY-184823CAS No.: 1417634-25-3CK2-IN-17 is a protein kinase CK2 inhibitor with an IC50 of 9.5 μM against human targets. CK2-IN-17 regulates the activity of protein kinase CK2 by interacting with its ATP-binding site. CK2-IN-17 can be used in studies related to protein kinase CK2-mediated pathways, such as tumors.
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CK2-TN03
0 ImagesCK2-TN03 is an ATP-competitive casein kinase 2 (CK2) inhibitor, with an IC50 of 165 nM and a Ki of 20 nM. CK2-TN03 inhibits CK2-mediated survivin activation and reduces CK2-dependent phosphorylation levels of BRD4/MYCN and AKT1. CK2-TN03 exerts anti-neuroblastoma effects by inhibiting survivin, leading to mitotic catastrophe and apoptosis of cancer cells. CK2-TN03 can be used in studies related to neuroblastoma.
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BioE-1115
0 ImagesBioE-1115 is a highly selective and potent PAS kinase (PASK) inhibitor with an IC50 of ~4 nM. BioE-1115 is also a potent casein kinase 2α inhibitor with an IC50 of ~10 μM.
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Hematein
0 ImagesHematein is a oxidation product of hematoxylin acted as a dye. Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells.
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CK2/ERK8-IN-1
0 ImagesCK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 (MAPK15, ERK7) inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy.
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Casein Kinase 2 Substrate Peptide
0 ImagesCasein Kinase 2 Substrate Peptide is a common CK2 substrate peptide. Casein Kinase 2 Substrate Peptide is synthesized with its C-terminus conjugated to 5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid (EDANS). Casein Kinase 2 Substrate Peptide can be used for protein kinase CK2 activity determination.
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CK2 inhibitor 2
0 ImagesCK2 inhibitor 2 is a potent, selective and orally active inhibitor of CK2, with an IC50 of 0.66 nM. CK2 inhibitor 2 shows high selectivity for Clk2 (IC50=32.69 nM)/CK2. CK2 inhibitor 2 exhibits favorable antiproliferative and antitumor activity.
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ON 108600
0 ImagesSynonyms: 108600ON 108600 (108600) is a CK2 (CK2α1: IC50 = 50 nM; CK2α2 = 5 nM), TNIK (IC50 = 5 nM) and DYRK (DYRK1A: IC50 = 16 nM; DYRK1B = 7 nM; DYRK2: = 28 nM). ON 108600 suppresses the growth of CD44high/CD24low breast cancer stem cell (BCSC) populations, induces G2/M arrest and apoptosis in triple negative breast cancer (TNBC) cells, and inhibits tubulin polymerization. ON 108600 can be used for the study of chemotherapy-resistant and metastatic TNBC.
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PI-828
0 ImagesPI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively.
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Quinalizarin
0 ImagesQuinalizarin is a protein kinase CK2 inhibitor with a Ki of 0.052 μM. Quinalizarin exhibits antifungal and anticancer activities. Quinalizarin induces ROS production, apoptotic signaling, mitochondrial pathway activation, cell cycle arrest, and cytotoxicity in cancer cells. Quinalizarin inhibits hyphal growth, biofilm formation, and mature biofilm integrity of Candida albicans. Quinalizarin can be used in research related to cancer and fungal infections.
