2. Signaling Pathways
  3. Cell Cycle/DNA Damage
    Stem Cell/Wnt
  4. Casein Kinase

Casein Kinase

Casein Kinase

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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:

Casein Kinase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-170860
    CK1δ/CK1ε liagnd-1
    		Ligand
    CK1δ/CK1ε liagnd-1 is the ligand for CK1δ/CK1ε that can be used for synthesis of CK1 PROTAC degrader AH078 (HY-170859) as the ligand for target protein.
    CK1δ/CK1ε liagnd-1
  • HY-168517
    PIM-1/CK2-IN-2
    		Inhibitor
    PIM-1/CK2-IN-2 (compound 3aA) is a PIM-1/CK2 inhibitor. PIM-1/CK2-IN-2 can induce the mitochondrial apoptotic pathway in CCRF-CEM cells. PIM-1/CK2-IN-2 can be used in cancer research.
    PIM-1/CK2-IN-2
  • HY-156040
    Casein kinase 1δ-IN-10
    		Inhibitor
    Casein kinase 1δ-IN-10 is a casein kinase 1δ (CK1δ) inhibitor (WO2012080729A2; compound 685).
    Casein kinase 1δ-IN-10
  • HY-120267
    TID43
    		Inhibitor
    TID43 is a CK2 inhibitor, with an IC50 of 0.3 μM. TID43 can be used for anti-angiogenic research.
    TID43
  • HY-128433
    CK1-IN-3
    		Inhibitor 99.00%
    CK1-IN-3 (compound 51) is a AC1 inhibitor with an IC50s 2.22 µM for CK-1δ.
    CK1-IN-3
  • HY-158370
    CK2-IN-11
    		Inhibitor
    CK2-IN-11 (32) is an allosteric CK2 inhibitor, with high selectivity for CK2 with IC50 values of 19.3 nM and 15.6 nM for the CK2α2β2 and the CK2α′2β2 isoforms, respectively.
    CK2-IN-11
  • HY-170859A
    AH081
    		Inhibitor
    AH081 (Compound 38) is a CK1δ/ε PROTAC degrader. AH081 is the negative control compound of AH078 (HY-170859). AH081 has inhibitory but no degradation activity for CK1δ/ε by using an inactive stereoisomer of the VHL ligand. Pink: CK1δ/ε ligand (HY-148251); Blue: VHL ligase ligand (HY-125845B); Black: linker
    AH081
  • HY-135816
    CK2/PIM1-IN-1
    		Inhibitor
    CK2/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.
    CK2/PIM1-IN-1
  • HY-162756
    CK1-IN-4
    		Inhibitor
    CK1-IN-4 (Compound 59) is an inhibitor for casein kinase CK1δ with IC50 of 2.74 μM. CK1-IN-4 exhibits neuroprotective effect in Ethacrynic acid (HY-B1640)-treated SH-SY5Y cells.
    CK1-IN-4
  • HY-49459
    Casein kinase 1δ-IN-14
    		Inhibitor 98.0%
    Casein kinase 1δ-IN-14 (compound 481) is a casein kinase inhibitor that can be used to study neurodegenerative diseases such as Alzheimer's disease.
    Casein kinase 1δ-IN-14
  • HY-169573
    Casein kinase 1δ-IN-16
    		Inhibitor
    Casein kinase 1δ-IN-16 (compound 506) is a casein kinase 1δ (CK1δ) inhibitor. Casein kinase 1δ-IN-16 can be utilized in neurodegenerative disorders research.
    Casein kinase 1δ-IN-16
  • HY-176508
    KDX1381
    		Inhibitor
    KDX1381 is a bivalent CK2α inhibitor (IC50: 17 nM, KD: 54 nM). KDX1381 has antitumor activity in mouse 786-O and A375 tumor xenograft models. KDX1381 combined with VEGFR inhibitors or DNA damaging agents enhances antitumor efficacy in mouse hepatocellular carcinoma and glioma models.
    KDX1381
  • HY-174347
    Hsp90-Cdc37-IN-4
    		Inhibitor
    Hsp90-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.
    Hsp90-Cdc37-IN-4
  • HY-P3921
    Casein Kinase II Substrate
    Casein Kinase II Substrate is a casein kinase II (CK2) peptide substrate that can be selectively phosphorylated by CK2.
    Casein Kinase II Substrate
  • HY-121792
    CK2-IN-1
    		Inhibitor
    CK2-IN-1 is a CK2 inhibitor, with an IC50 of 150 nM.
    CK2-IN-1
  • HY-108642A
    AMG-548 hydrochloride
    		Inhibitor
    AMG-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.
    AMG-548 hydrochloride
  • HY-176561
    IOR-160
    		Inhibitor
    IOR-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.
    IOR-160
  • HY-W842364
    CK1δ-IN-3
    		Inhibitor
    CK1δ-IN-3 (compound 376) is a casein kinase 1δ (CK1δ) inhibitor. CK1δ-IN-3 can be utilized in neurodegenerative disorders research.
    CK1δ-IN-3
  • HY-169706
    Casein kinase 1δ-IN-25
    		Inhibitor
    Casein 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.
    Casein kinase 1δ-IN-25
  • HY-125865A
    Human casein
    Human casein is an orally active phosphoprotein that can be separated into various electrophoretic components, such as α2-Casein, κ-Casein, β-casein, and γ-casein. Human casein has also been blended and grafted with other polymers, cross-linkers, or monomers to improve its functional properties. Human casein enhances calcium absorption and reduces the extent of fissure as well as smooth-surface caries. Human casein promotes proliferation of prostate cancer. Human casein has various applications in the paper, leather, textile, and food industries, serving as coatings, adhesives, and packaging materials.
    Human casein
Cat. No. Product Name / Synonyms Application Reactivity
Casein Kinase Isoform Comparison

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