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-157478
    CSNK2A-IN-1
    		Inhibitor 98.46%
    CSNK2A-IN-1 (compound 7C) is a selective CSNK2A inhibitor. CSNK2A-IN-1 has antiviral activity and improved selectivity over PIM3.
    CSNK2A-IN-1
  • HY-12279C
    Umbralisib hydrochloride
    		Inhibitor 99.04%
    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-145260
    BRD4/CK2-IN-1
    		Inhibitor 98.21%
    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-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-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-111378
    Casein Kinase II Inhibitor IV
    		Inhibitor 98.0%
    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-148318
    CK2α-IN-1
    		Inhibitor 98.34%
    CK2α-IN-1 (compound 2) is a selective CK2α inhibitor (IC50=7.0 µM; Ki=1.6 µM) that exhibits a non-ATP-competitive mode of action. CK2α-IN-1 exhibits good potential for anticancer studies.
    CK2α-IN-1
  • HY-128677
    NCC007
    		Inhibitor 99.22%
    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-148233S
    JNJ-6204
    		99.75%
    JNJ-6204 is a dual inhibitor for CSNK1D (Casein Kinase 1 Delta) and CSNK1E (Casein Kinase 1 Epsilon) (CSNK1D IC50=2.3 nM; CSNK1E IC50=137 nM). JNJ-6204 shows good brain exposure.
    JNJ-6204
  • HY-103383
    (R)-DRF053 dihydrochloride
    		Inhibitor 99.30%
    (R)-DRF053 dihydrochloride is a potent casein kinases 1 (CK1), CDK1/cyclin B and CDK5/p25 inhibitor with IC50s of 14 nM, 220 nM and 80 nM, respectively. (R)-DRF053 dihydrochloride prevents the CK1-dependent production of amyloid-beta in a cell model.
    (R)-DRF053 dihydrochloride
  • HY-148489
    CSNK1-IN-1
    		Inhibitor 99.23%
    CSNK1-IN-1 is a CSNK1A1 inhibitor. CSNK1-IN-1 has inhibitory activity for CSNK1A1 kinase with IC50 values of 21 μM. CSNK1-IN-1 can be used for the research of proliferative disorders.
    CSNK1-IN-1
  • HY-158369
    CK2-IN-10
    		99.70%
    CK2-IN-10 (31), an allosteric CK2 inhibitor, can be used in the research of cancer.
    CK2-IN-10
  • HY-148455
    Casein kinase 1δ-IN-3
    		Inhibitor 99.50%
    Casein kinase 1δ-IN-3 (Compound 23a) is a casein kinase 1 delta (CK1d) inhibitor with a pIC50 of 6.5376 M.
    Casein kinase 1δ-IN-3
  • HY-168615
    MGD-28
    		Degrader 99.73%
    MGD-28 is a potent, orally active, Cereblon (CRBN)-dependent IKAROS protein degrader that degrades IKZF1 (DC50=3.8 nM), IKZF2 (DC50=56.3 nM), and IKZF3 (DC50=7.1 nM) in a dose-dependent manner. In addition, MGD-4 also degrades CK1α (DC50=7.8 nM). MGD-28 has antiproliferative activity and can be used in multiple myeloma research.
    MGD-28
  • HY-117857
    MRT00033659
    		Inhibitor 99.77%
    MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC50=0.9 μM for CK1δ) and CHK1 (IC50=0.23 μM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation.
    MRT00033659
  • HY-50733A
    CX-5011
    		Inhibitor 99.48%
    CX-5011 is a CK2 inhibitor. CX-5011 also induces Rac1 activation. CX-5011 induces apoptosis and induces cancer cell death.
    CX-5011
  • HY-P4056A
    CIGB-300 acetate
    		Antagonist 98.00%
    CIGB-300 acetate (P15-Tat acetate) is an anti-casein kinase 2 (CK2) peptide that exhibits anticancer properties by interfering with the phosphorylation of protein kinase CK2. CIGB-300 acetate induces apoptosis in multiple tumor cell lines and can be used in cancer research.
    CIGB-300 acetate
  • HY-121944
    Ricinine
    		Inhibitor 99.81%
    Ricinine exhibits hepatoprotection in CCl4-induced liver damage. Ricinine is also a CK1α inhibitor, and may activate Wnt pathway.
    Ricinine
  • HY-169347
    dCK1α-2
    		Degrader
    dCK1α-2 is an orally active CK1α molecular glue degrader that targets p53 pathway-related targets. dCK1α-2 exhibits anti-tumor efficacy in mouse models and can increase the expression of p53-related genes..
    dCK1α-2
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Casein Kinase Isoform Comparison

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