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-15535
    DMAT
    		Inhibitor 98.09%
    DMAT is a potent and specific CK2 inhibitor with an IC50 value of 130 nM.
    DMAT
  • HY-139004
    SGC-CK2-1
    		Inhibitor 99.67%
    SGC-CK2-1 is a highly potent, ATP-competitive, and cell-active CK2 chemical probe with exclusive selectivity for both human CK2 isoforms, with IC50s of 36 and 16 nM for CK2α and CK2α′respectively in the nanoBRET assay. SGC-CK2-1 can be used for the research of neurodegenerative diseases.
    SGC-CK2-1
  • HY-12774
    IC261
    		Inhibitor 99.54%
    IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively.
    IC261
  • HY-120675
    SSTC3
    		Activator 98.65%
    SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
    SSTC3
  • HY-108642B
    AMG-548 dihydrochloride
    		Inhibitor 99.91%
    AMG-548 dihydrochloride, 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 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
    AMG-548 dihydrochloride
  • HY-115519
    (E/Z)-GO289
    		Inhibitor 99.60%
    (E/Z)-GO289 is a potent and selective casein kinase 2 (CK2) inhibitor (IC50=7 nM). (E/Z)-GO289 strongly lengthens circadian period. (E/Z)-GO289 exhibits cell type–dependent inhibition of cancer cell growth that correlated with cellular clock function.
    (E/Z)-GO289
  • HY-10456
    TAK-715
    		Inhibitor 99.76%
    TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model.
    TAK-715
  • HY-12443
    PF-5006739
    		Inhibitor 99.56%
    PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid agent-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner. PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity.
    PF-5006739
  • HY-133028
    CKI-7 free base
    		Inhibitor 99.80%
    CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases.
    CKI-7 free base
  • HY-145939
    BAY-888
    		Inhibitor 98.35%
    BAY-888 is an orally active CSNK1A1 and CSNK1D inhibitor with IC50 of 1.5 nM and 5.5 nM, respectively. BAY-888 has antitumor activity.
    BAY-888
  • HY-129571
    BioE-1115
    		Inhibitor 99.56%
    BioE-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.
    BioE-1115
  • HY-125865
    Casein
    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. Casein has also been blended and grafted with other polymers, cross-linkers, or monomers to improve its functional properties. Casein enhances calcium absorption and reduces the extent of fissure as well as smooth-surface caries. Casein promotes proliferation of prostate cancer. Casein has various applications in the paper, leather, textile, and food industries, serving as coatings, adhesives, and packaging materials.
    Casein
  • HY-135906
    CK2/ERK8-IN-1
    		Inhibitor ≥99.0%
    CK2/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.
    CK2/ERK8-IN-1
  • HY-15479
    TTP 22
    		Inhibitor 98.40%
    TTP 22 is a potent CK2 inhibitor, with an IC50 of 100 nM and a Ki of 40 nM.
    TTP 22
  • HY-10108A
    LY294002 hydrochloride
    		Inhibitor 99.93%
    LY294002 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.
    LY294002 hydrochloride
  • HY-114858
    Epiblastin A
    		Inhibitor 99.51%
    Epiblastin A is an ATP competitive casein kinase 1 (CK1) inhibitor with IC50s of 8.9, 0.5, and 4.7 µM for CK1α, CK1δ, and CK1 ɛ, respectively. Epiblastin A induces reprogramming of epiblast stem cells into embryonic stem cells by inhibition of CK1.
    Epiblastin A
  • HY-145940
    BAY-204
    		Inhibitor 99.94%
    BAY-204 is an inhibitor of Casein kinase 1 alpha and delta (CSNK1α and δ) useful for the research of proliferative disorders.
    BAY-204
  • HY-119751
    Hematein
    		Inhibitor
    Hematein 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.
    Hematein
  • HY-111820
    CK1-IN-1
    		Inhibitor 99.35%
    CK1-IN-1 is a casein kinase 1 (CK1) inhibitor extracted from patent WO2015119579A1, compound 1c, has IC50s of 15 nM, 16 nM, 73 nM for CK1δ, and CK1ε, p38σ MAPK, respectively.
    CK1-IN-1
  • HY-120084
    BTX161
    		Inhibitor 99.20%
    BTX161, a thalidomide analog, is an effective CKIα degrader. BTX161 mediates human AML cell CKIα degradation more effectively than lenalidomide and activates the DNA damage response (DDR) and p53, while stabilizing p53 antagonist MDM2.
    BTX161
Cat. No. Product Name / Synonyms Application Reactivity
Casein Kinase Isoform Comparison

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