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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BRD4/CK2-IN-1
0 ImagesBRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
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A-3 hydrochloride
0 ImagesA-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
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APL-5125
0 ImagesCat. No.: HY-178980CAS No.: 2830619-57-1APL-5125 (Compound 61f) is a potent, selective and orally active ATP-competitive CK2α inhibitor with an IC50 of 0.348 nM and a Ki of 0.095 nM. APL-5125 binds to CK2α in a bivalent manner, simultaneously interacting with the ATP-binding site and the αD pocket. APL-5125 exhibits antitumor activity and can be used for the research of cancer, such as colon cancer.
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IQA
0 ImagesCat. No.: HY-117332CAS No.: 391670-48-7Synonyms: CGP-029482IQA (CGP-029482) is a potent and selective protein kinase CK2 inhibitor.
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Casein Kinase II Receptor Peptide
0 ImagesCat. No.: HY-P3748CAS No.: 198481-81-1Casein Kinase II Receptor Peptide is a substrate for casein kinase II with an Km value of 500 µM. Casein Kinase II Substrate can be used for measure casein kinase II activity in crude enzyme preparations.
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CK2-IN-15
0 ImagesCat. No.: HY-174350CK2-IN-15 (Compound Biv5) is a selective and potent bivalent protein kinase CK2 inhibitor with an IC50 value of 51 pM. CK2-IN-15 significantly reduces the replication of SARS-CoV-2 in HEK-ACE2-TMPRSS2 and Vero cells, and also reduces viral replication in an ex vivo model of human nasal epithelial cells. CK2-IN-15 is promising for research of β-coronavirus infection-related diseases.
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CK2 Substrate peptide
0 ImagesCat. No.: HY-P11496CAS No.: 154444-98-1CK2 Substrate peptide (Compound RRRADDSDDDDD) is a specific CK2 peptide substrate with Km of 13 μM. CK2 Substrate peptide can be used for the research of neurological disease, such as Alzheimer's Disease.
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CK2-IN-3
0 ImagesCat. No.: HY-151382CAS No.: 2969205-85-2CK2-IN-3 is a selective and potent CK2 inhibitor (Kd: 12 nM), with IC50 values of 1.51 μM (CK2α) and 7.64 μM (CK2α’). CK2-IN-3 can be used in the research of cancers.
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BMS-159
0 ImagesCat. No.: HY-180987CAS No.: 1541248-45-6
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TID43
0 ImagesCat. No.: HY-120267CAS No.: 19231-60-8TID43 is a CK2 inhibitor, with an IC50 of 0.3 μM. TID43 can be used for anti-angiogenic research.
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CK2/PIM1-IN-1
0 ImagesCat. No.: HY-135816CAS No.: 292640-28-9CK2/PIM1-IN-1 is an inhibitor of CK2 and PIM1, with IC50s of 3.787 μM and 4.327 μM for CK2 and PIM1, respectively. CK2/PIM1-IN-1 is developed for the research of proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders.
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BMS-135
0 ImagesCat. No.: HY-181022CAS No.: 1541248-36-5BMS-135 is a potenr, selective and ATP-competitive casein kinase 2 (CK2) inhibitor with IC50 of 0.8 and 0.3 nM for CK2αandCK2α′ isoforms. BMS-135 can simulate the structure of ATP and bind to the active pocket of CK2, thereby inhibiting its serine/threonine phosphorylation function. BMS-135 can inhibit cells proliferation and shows anti-tumor effect. BMS-135 can be used for research of colon cancer.
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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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IOR-160
0 ImagesCat. No.: HY-176561CAS No.: 2421119-78-8IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDACs. IOR-160 exhibits high selectivity for CK2 (IC50 = 1.7 nM) and broad inhibitory activity against HDAC (HDAC 1, 2, 3, and 6 with IC50s of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, with low activity for HDAC8). IOR-160 modulates key cellular signaling pathways by inhibiting AKT phosphorylation and increasing acetylated α-tubulin. IOR-160 inhibits tumor growth and reduces tumor burden through dual CK2/HDAC inhibition. IOR-160 is indicated for use in triple-negative breast cancer research.
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CK2 inhibitor 4
0 ImagesCat. No.: HY-169629CAS No.: 474263-21-3CK2 inhibitor 4 (compound 5b) is a protein kinase CK2 inhibitor with IC50 of 3.8 μM. CK2 inhibitor 4 can be used in tumor research.
