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 (57)
Related Products (57)
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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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LY294002 hydrochloride
0 ImagesLY294002 hydrochloride is a potent and broad-spectrum PI3K inhibitor, with IC50 values of 0.5, 0.57, and 0.97 μM for P110α, P110δ and P110β, respectively. LY294002 hydrochloride also inhibits CK2 with an IC50 of 98 nM. LY294002 hydrochloride can be used for pancreatic cancer research.
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Emodin (Standard)
0 ImagesEmodin (Standard) is the analytical standard of Emodin. This product is intended for research and analytical applications. Emodin (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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CX-5011
0 ImagesCX-5011 is an ATP-competitive, selective CK2 inhibitor with an IC50 of 0.97 nM for nCK2. CX-5011 reduces Bin1, CKB, Tubb3, and Pxn levels. CX-5011 impairs myogenic differentiation, myotube formation, muscle markers, myofiber growth, and zebrafish muscle development/locomotion. CX-5011 can be used for breast cancer research.
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CX-5011 free base
0 ImagesCat. No.: HY-50733CAS No.: 1009821-06-0CX-5011 free base is an ATP-competitive, selective CK2 inhibitor with an IC50 of 0.97 nM for nCK2. CX-5011 free base reduces Bin1, CKB, Tubb3, and Pxn levels. CX-5011 free base impairs myogenic differentiation, myotube formation, muscle markers, myofiber growth, and zebrafish muscle development/locomotion. CX-5011 free base can be used for breast cancer research.
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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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TBCA
0 ImagesTBCA is a highly selective CK2 (casein kinase II) inhibitor with an IC50 of 110 nM and a Ki of 77 nM. TBCA shows selectivity for CK2 over CK1, DYRK1A and a panel of 27 other kinases.
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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.
