Casein Kinase
Casein Kinases (CKs), a group of ubiquitous Ser/Thr kinases, regulate a wide range of cellular functions in eukaryotes, including phosphorylation of proteins that are substrates for degradation via the ubiquitin-proteasome system (UPS). Two casein kinases, casein kinase-1 (CK-1) and casein kinase-2 (CK-2), have been characterized from many sources.
CK1 kinases exist in at least seven isoforms (α, β, γ1-3, δ, and ɛ) in mammals and CK1 kinases phosphorylate various substrates to play vital roles in diverse physiological processes such as DNA repair, cell cycle progression, cytokinesis, differentiation, and apoptosis. Casein kinase 2 (CK2) is a highly pleiotropic serine-threonine kinase, which catalyzed phosphorylation of more than 300 proteins that are implicated in regulation of many cellular functions, such as signal transduction, transcriptional control, apoptosis, and the cell cycle.
Casein Kinase Isoform Specific Products
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Casein Kinase Inhibitors
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Casein Kinase Antagonists
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Casein Kinase Activator
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Casein Kinase Chemical
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Casein Kinase Degraders
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Casein Kinase Substrate
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Casein Kinase Ligand
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Casein Kinase Related Products (247)
Related Products (247)
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Antibodies (5)
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Casein Kinase Isoform Comparison
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PF-5236216
0 ImagesCat. No.: HY-135629CAS No.: 1383376-93-9PF-5236216 is a brain-penetrant CK1δ/CK1ε inhibitor with IC50 values of 8 and 36 nM. PF-5236216 inhibits CK1δ and CK1ε-mediated PER3 nuclear translocation. PF-5236216 forms an H-bond with the backbone NH of Leu85, hydrophobic stacking with Met82, and a water-mediated H-bond with Lys38 of CK1δ. PF-5236216 can be used as a tool ligand for CNS PET studies.
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Hsp90-Cdc37-IN-4
0 ImagesCat. No.: HY-174347CAS No.: 2758818-41-4Hsp90-Cdc37-IN-4, a Celastrol (HY-13067) derivative, inhibits the Hsp90-Cdc37 protein-protein interaction (PPI). Hsp90-Cdc37-IN-4 selectively inhibits casein kinase 2 (CK2), reducing phosphorylation of its substrate Cdc37 at Serine 13. Hsp90-Cdc37-IN-4 induces G0/G1 cell cycle arrest and triggers apoptosis via the mitochondrial pathway. Hsp90-Cdc37-IN-4 demonstrates potent anti-breast cancer activity.
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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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Casein Kinase II Substrate
0 ImagesCasein Kinase II Substrate is a casein kinase II (CK2) peptide substrate that can be selectively phosphorylated by CK2.
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CK1δ-IN-1
0 ImagesCat. No.: HY-164578CAS No.: 352555-07-8CK1δ-IN-1 (example 939) is a casein kinase 1 delta (CK1δ) inhibitor. CK1δ-IN-1 can be used for the study of Alzheimer's disease.
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rac-Lenalidomide-13C5
0 ImagesCat. No.: HY-W777286CAS No.: 1219332-91-8Synonyms: CC-5013-13C5rac-Lenalidomide-13C5 (CC-5013-13C5) is the 13C5-labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013) is an orally active immunomodulatory agent that binds CRBN as a molecular glue to alter substrate specificity, inducing ubiquitination and proteasome-dependent degradation of IKZF1, IKZF3 and CK1α. Lenalidomide induces apoptosis by degrading IKZF1/3, and activates p53 by degrading CK1α. Lenalidomide promotes IL-2 release and effector functions of CD8+ T/NK cells, while inhibiting TNF-α secretion and M1-type pyroptosis. Lenalidomide can be used in research related to hematological malignancies, acute liver failure and acute kidney injury.
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CK1γ-IN-1
0 ImagesCat. No.: HY-181586CAS No.: 1397706-29-4
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AMG-548 hydrochloride
0 ImagesCat. No.: HY-108642ACAS No.: 2437438-16-7AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
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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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BMS-135-L-Lys
0 ImagesCat. No.: HY-184414BMS-135-L-Lys is a dual-cation prodrug derived from CK2 inhibitor BMS-135 (HY-181022) through esterification with L-lysine using a secondary alcohol. BMS-135-L-Lys achieves enhanced solubility by maintaining protonation of the ε-amino group of the Lys side chain at intestinal pH. BMS-135-L-Lys is released in situ by intestinal wall esterase from the parent drug, significantly increasing the oral bioavailability of the parent drug and overcoming the non-linear pharmacokinetic problem when the dose of the parent drug is increased. BMS-135-L-Lys can be used in related research on colon cancer and lung cancer.
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CK1δ-IN-3
0 ImagesCat. No.: HY-W842364CAS No.: 571174-12-4CK1δ-IN-3 (compound 376) is a casein kinase 1δ (CK1δ) inhibitor. CK1δ-IN-3 can be utilized in neurodegenerative disorders research.
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Casein kinase 1δ-IN-25
0 ImagesCat. No.: HY-169706CAS No.: 753468-25-6Casein kinase 1δ-IN-25 (compound 487) is a potent casein kinase 1δ inhibitor. Casein kinase 1δ-IN-25 can be used in the study of neurodegenerative diseases such as Alzheimer's disease.
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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.
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MU1742-amide-C6-acid
0 ImagesCat. No.: HY-176825MU1742-amide-C6-acid is a CK1δ/ε inhibitor. MU1742-amide-C6-acid can be used for synthesis of PROTAC AH081 (HY-170859A).
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Casein kinase 1δ-IN-28
0 ImagesCat. No.: HY-171278CAS No.: 1095750-94-9Casein kinase 1δ-IN-28 (Compound 4) is the inhibitor for CK1ε with an IC50 of 0.0146 μM. Casein kinase 1δ-IN-28 exhibits a metabolite rate in human liver microsomes of 52%.
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LRRK2/JNK3-IN-1
0 ImagesCat. No.: HY-184652LRRK2/JNK3-IN-1 is a brain-penetrant multi-target inhibitor of LRRK2 (including G2019S mutant and wild-type) and JNK3, with enzymatic IC50 values of 3.90 nM against LRRK2G2019S, 3.24 nM against wild-type LRRK2, and 22.1 nM against JNK3. LRRK2/JNK3-IN-1 displays favorable selectivity in a 97-kinase profiling screen, and also shows inhibitory activity against JNK1, JNK2, and MKNK2. LRRK2/JNK3-IN-1 can be used for the research of Parkinson's disease.
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(E/Z)-Chk2-IN-1
0 ImagesCat. No.: HY-112477ACAS No.: 693222-51-4Synonyms: (E/Z)-Hymenialdisine analogue-1(E/Z)-Chk2-IN-1 ((E/Z)-Hymenialdisine analogue-1) (Compound 1) is a potent and selective cell cycle kinase Chk2 inhibitor with an IC50 of 8 nM. (E/Z)-Chk2-IN-1 exhibits low inhibitory activity against other kinases (such as CK1δ, MEK1, and PKCα/βⅡ) with IC50 values both >89 nM. (E/Z)-Chk2-IN-1 can be used for the research of cancer.
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CK1α-IN-1
0 ImagesCat. No.: HY-181048CK1α-IN-1 (Compound 7a) is a selective CK1α inhibitor with an IC50 of 10.96 nM. CK1α-IN-1 dose-dependently stabilizes p53 protein. CK1α-IN-1 has anticancer activity against acute monocytic leukemia.
