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-160444
    SJ3149
    		Degrader 99.48%
    SJ3149 is a selective and potent in vitro and in vivo degrader of CK1α protein with broad antiproliferative activity. SJ3149 can be used in cancer research.
    SJ3149
  • 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-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-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-133028
    CKI-7 free base
    		Inhibitor 99.34%
    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-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-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-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-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 98.03%
    TTP 22 is a potent CK2 inhibitor, with an IC50 of 100 nM and a Ki of 40 nM.
    TTP 22
  • 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-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-100114
    TA-01
    		Inhibitor 99.86%
    TA-01 is a potent CK1 and p38 MAPK inhibitor, with IC50s of 6.4 nM, 6.8 nM, 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively. TA-01 acts as a cardiogenic inhibitor.
    TA-01
  • HY-128677
    NCC007
    		Inhibitor 99.73%
    NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor with IC50s of 1.8 and 3.6 μM, respectively. NCC007 can be used in research of modulating mammalian circadian rhythms.
    NCC007
  • HY-120084
    BTX161
    		Inhibitor 98.58%
    BTX161, a Thalidomide analog, is a potent CKIα degrader. BTX161 mediates degradation of CKIα better than Lenalidomide in human AML cells and activates DNA damage response (DDR) and p53, while stabilizing the p53 antagonist MDM2.
    BTX161
  • HY-123955
    Casein Kinase inhibitor A86
    		Inhibitor 99.26%
    Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb). Casein Kinase inhibitor A861 induces leukemia cell apoptosis, and has potent anti-leukemic activities.
    Casein Kinase inhibitor A86
  • HY-P3815
    Casein Kinase 2 Substrate Peptide
    		98.47%
    Casein Kinase 2 Substrate Peptide is a common CK2 substrate peptide. Casein Kinase 2 Substrate Peptide is synthesized with its C-terminus conjugated to 5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid (EDANS). Casein Kinase 2 Substrate Peptide can be used for protein kinase CK2 activity determination.
    Casein Kinase 2 Substrate Peptide
  • HY-157334
    DEG-77
    		98.31%
    DEG-77, a PROTAC based IKZF2 and CK1α degrader, possesses suitable pharmacokinetic properties, solubility, and selectivity for in vivo studies (t1/2=8h).
    DEG-77
Cat. No. Product Name / Synonyms Application Reactivity
Casein Kinase Isoform Comparison

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