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-15704
    LH846
    		Inhibitor 98.04%
    LH846 is a selective inhibitor of CKIδ, with an IC50 of 290 nM, and less potently inhibits CKIα and CKIε, with IC50s of 2.5 μM and 1.3 μM, respectively.
    LH846
  • HY-111378
    Casein Kinase II Inhibitor IV
    		Inhibitor 98.01%
    Casein Kinase II Inhibitor IV is a potent, ATP-competitive of casein kinase II inhibitor with an IC50 of 9 nM. Casein Kinase II Inhibitor IV ia also a human keratinocytes (NHEK) differentiation inducer.
    Casein Kinase II Inhibitor IV
  • HY-148251
    MU1742
    		99.74%
    MU1742 is a probe for CK1δ and CK1ε protein kinases.
    MU1742
  • HY-12279C
    Umbralisib hydrochloride
    		Inhibitor 98.98%
    Umbralisib (TGR-1202) hydrochloride is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach.
    Umbralisib hydrochloride
  • HY-108606
    PI-828
    		Inhibitor 99.09%
    PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively.
    PI-828
  • 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-132175
    CK2 inhibitor 2
    		Inhibitor 98.51%
    CK2 inhibitor 2 is a potent, selective and orally active inhibitor of CK2, with an IC50 of 0.66 nM. CK2 inhibitor 2 shows high selectivity for Clk2 (IC50=32.69 nM)/CK2. CK2 inhibitor 2 exhibits favorable antiproliferative and antitumor activity.
    CK2 inhibitor 2
  • HY-153905
    Casein kinase 1δ-IN-6
    		Inhibitor 99.93%
    Casein kinase 1δ-IN-6 is a potent and selective protein kinase CK-1δ inhibitor with an IC50 of 23 nM. Casein kinase 1δ-IN-6 shows neuroprotective and anti-inflammatory properties both in vitro and in vivo. Casein kinase 1δ-IN-6 is a promising drug candidate and can be used for neurodegenerative diseases research.
    Casein kinase 1δ-IN-6
  • HY-110052
    TBCA
    		Inhibitor 99.60%
    TBCA is a highly selective CK2 (casein kinase II) inhibitor with an IC50 of 110 nM and a Ki of 77 nM. TBCA shows selectivity for CK2 over CK1, DYRK1A and a panel of 27 other kinases.
    TBCA
  • HY-114653
    SRPIN803
    		Inhibitor 99.17%
    SRPIN803 is a potent CK2 and SRPK1 dual inhibitor, with IC50s of 203 nM and 2.4 μM, respectively. SRPIN803 exhibits antiangiogenic activity. SRPIN803 can be used for the research of age-related macular degeneration.
    SRPIN803
  • HY-125957
    A-3 hydrochloride
    		Inhibitor 99.75%
    A-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.
    A-3 hydrochloride
  • HY-156816
    ON 108600
    		Inhibitor 99.73%
    ON 108600 is a inhibitor for CK2 (Casein Kinase2)/TNIK/DYRK1 , with the IC50s for DYRK1A/DYRKB, DYRK2, CK2α1/CK2α2, and TNIK of 0.016 μm/0.007 μM, 0.028 μM, 0.05 μM/0.005 μM, and 0.005 μM, respectively. ON 108600 has antitumor activity.
    ON 108600
  • HY-N3127
    Orobol
    		Inhibitor 99.28%
    Orobol is one of the major soy isoflavones and has various pharmacological activities, including anti-skin-aging and anti-obesity effects. Orobol inhibits CK1ε, VEGFR2/KDR/Flk-1, MAP4K5, MNK1, MUSK, TOPK, and TNIK (IC50=1.24-4.45 μM). Orobol also inhibits PI3K isoforms (IC50=3.46-5.27 μM for PI3K α/β/γ/K/δ).
    Orobol
  • HY-145260
    BRD4/CK2-IN-1
    		Inhibitor 98.62%
    BRD4/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)
    BRD4/CK2-IN-1
  • HY-156666
    Casein kinase 1δ-IN-8
    		≥98.0%
    Casein kinase 1δ-IN-8 (compound 494) is an inhibitor of Casein kinase 1δ, Casein kinase 1δ-IN-8 can be used in the treatment of neurodegenerative disorders such as Alzheimer's disease[1].
    Casein kinase 1δ-IN-8
  • HY-148112
    Casein kinase 1δ-IN-1
    		Inhibitor 99.91%
    Casein kinase 1δ-IN-1 (compound 822) is an inhibitor of casein kinase 1 delta (CK1δ), exhibits inhibition of greater than 5%. Casein kinase 1δ-IN-1 can be used for neurodegenerative disorders such as Alzheimer's disease research.
    Casein kinase 1δ-IN-1
  • HY-108642
    AMG-548
    		Inhibitor ≥99.0%
    AMG-548, 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 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
    AMG-548
  • HY-111378A
    Casein Kinase II Inhibitor IV hydrochloride
    		Inhibitor
    Casein Kinase II Inhibitor IV Hydrochloride is a small-molecule inducer of epidermal keratinocyte differentiation.
    Casein Kinase II Inhibitor IV hydrochloride
  • HY-12279A
    Umbralisib tosylate
    		Inhibitor
    Umbralisib (TGR-1202) tosylate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach.
    Umbralisib tosylate
  • HY-12279B
    Umbralisib sulfate
    		Inhibitor
    Umbralisib (TGR-1202) sulfate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib sulfate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib sulfate can be used for haematological malignancies reseach.
    Umbralisib sulfate
Cat. No. Product Name / Synonyms Application Reactivity
Casein Kinase Isoform Comparison

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