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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EGFR-IN-57
0 ImagesCat. No.: HY-146138CAS No.: 2492382-37-1EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis.
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Multi-kinase-IN-6
0 ImagesCat. No.: HY-156470CAS No.: 3009081-73-3Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect.
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CAM4066
0 ImagesCat. No.: HY-123853CAS No.: 2101206-81-7
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CX-5279
0 ImagesCat. No.: HY-171744CAS No.: 1333382-32-3CX-5279 is an efficient and selective CK2 inhibitor with IC50 values for nCK2 and CK2α of 2.73 and 0.91 nM, respectively. CX-5279 is sensitive to mutations at Val66, Ile174, and V66I174AA, with IC50 values of 13.8, 12.5, and 23.35 nM, respectively. CX-5279's inhibitory activity against PIM1 is very weak, with a IC50 value of 8.52 μM. CX-5279 exhibits anti-proliferative activity in various cancer cell lines. CX-5279 can be used for research on cancers such as pancreatic cancer and leukemia.
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TMCB
0 ImagesCat. No.: HY-103384CAS No.: 905105-89-7TMCB is a selective, ATP-competitive CK2 (casein kinase II) inhibitor with distinct Ki values of 83 nM and 21 nM for the two different catalytic CK2 subunits α and α', respectively.
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CK2 inhibitor 3
0 ImagesCat. No.: HY-143461CAS No.: 2979847-14-6CK2 inhibitor 3 is a potent CK2 inhibitor with IC50 value of 280 nM. CK2 inhibitor 3 inhibits endocellular CK2, significantly affects viability of tumour cells and shows remarkable selectivity on a panel of 320 kinases.
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4,5,6,7-Tetrabromo-1H-benzimidazole
0 ImagesCat. No.: HY-W042648CAS No.: 577779-57-84,5,6,7-Tetrabromobenzimidazole is a selective and ATP competitive CK2 (casein kinase 2) inhibitor.
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CX-5279 free acid
0 ImagesCat. No.: HY-184458CAS No.: 1009821-64-0CX-5279 free acid is an efficient and selective CK2 inhibitor with IC50 values for nCK2 and CK2α of 2.73 and 0.91 nM, respectively. CX-5279 free acid is sensitive to mutations at Val66, Ile174, and V66I174AA, with IC50 values of 13.8, 12.5, and 23.35 nM, respectively. CX-5279 free acid's inhibitory activity against PIM1 is very weak, with a IC50 value of 8.52 μM. CX-5279 free acid exhibits anti-proliferative activity in various cancer cell lines. CX-5279 free acid can be used for research on cancers such as pancreatic cancer and leukemia.
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PLK1-IN-17
0 ImagesCat. No.: HY-184863CAS No.: 1034617-66-7PLK1-IN-17 is a potent PLK1 inhibitor with an IC50 of 2 nM. PLK1-IN-17 shows high selectivity for PLK2 and CDK2/A, moderate selectivity for PLK3, only weak activity against CK2, FLT3 and NEK6, and no activity against PDGFR, ALK and another 37 kinases. PLK1-IN-17 inhibits the proliferation of ovarian cancer cells and can be used in ovarian cancer-related research.
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CK2-IN-18
0 ImagesCat. No.: HY-184824CAS No.: 1417638-06-2CK2-IN-18 is a protein kinase CK2 inhibitor with an IC50 of > 30 μM against protein kinase CK2. CK2-IN-18 can be used in studies related to CK2-mediated signaling pathways, such as various cancers including lung cancer and breast cancer.
