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-10108
    LY294002
    		Inhibitor 99.95%
    LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an apoptosis activator.
    LY294002
  • HY-50855
    Silmitasertib
    		Inhibitor 99.94%
    Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
    Silmitasertib
  • HY-13912
    IWP-2
    		Inhibitor 99.51%
    IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC50 of 40 nM for the gatekeeper mutant M82FCK1δ.
    IWP-2
  • HY-14393
    Emodin
    		Inhibitor 99.20%
    Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice.
    Emodin
  • HY-B0183
    Ellagic acid
    		Inhibitor 99.23%
    Ellagic acid is a natural antioxidant, and acts as a potent and ATP-competitive inhibitor of CK2 and SHP2, with an IC50 of 40 nM and a Ki of 20 nM.
    Ellagic acid
  • HY-160444
    SJ3149
    		Degrader 99.40%
    SJ3149 is a selective and potent degrader of CK1α protein in vitro and in vivo. SJ3149 has antitumor activity.
    SJ3149
  • 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
  • HY-155987
    CK2-IN-8
    		Inhibitor
    CK2-IN-8 (compound 5c) is a CK2 inhibitor with IC50 >33 μM.
    CK2-IN-8
  • HY-10324
    D4476
    		Inhibitor 99.94%
    D4476 is a potent, selective and cell-permeable inhibitor of casein kinase 1(CK1) with an IC50 value of 0.3 μM in vitro.
    D4476
  • HY-15490
    PF-670462 dihydrochloride
    		Inhibitor 99.96%
    PF-670462 dihydrochloride is a potent and selective inhibitor of casein kinase (CK1ε and CK1δ), with IC50s of 7.7 nM and 14 nM, respectively.
    PF-670462 dihydrochloride
  • HY-12279
    Umbralisib
    		Inhibitor 98.69%
    Umbralisib (TGR-1202) 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 exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach.
    Umbralisib
  • HY-50855B
    Silmitasertib sodium salt
    		Inhibitor 99.91%
    Silmitasertib sodium salt is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
    Silmitasertib sodium salt
  • HY-14394
    TBB
    		Inhibitor 99.31%
    TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC50 of 0.15 μM for rat liver CK2.
    TBB
  • HY-145322
    TMX-4116
    		Inhibitor 99.50%
    TMX-4116 is a casein kinase 1α (CK1α) degrader. TMX-4116 shows the degradation preference for CK1α with DC50s less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4116 can be used for the research of multiple myeloma.
    TMX-4116
  • HY-123954
    Casein Kinase inhibitor A51
    		Inhibitor 98.42%
    Casein Kinase inhibitor A51 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A51 induces leukemia cell apoptosis, and has potent anti-leukemic activities.
    Casein Kinase inhibitor A51
  • HY-15535
    DMAT
    		Inhibitor 98.09%
    DMAT is a potent and specific CK2 inhibitor with an IC50 value of 130 nM.
    DMAT
  • HY-12470
    PF-4800567
    		Inhibitor 98.04%
    PF-4800567 is a potent and selective inhibitor of casein kinase 1ϵ (CK1ϵ), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM).
    PF-4800567
  • HY-100011
    SR-3029
    		Inhibitor 99.41%
    SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively, and Kis of 97 nM for both kinases.
    SR-3029
  • HY-115519
    (E/Z)-GO289
    		Inhibitor 99.72%
    (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-145319
    FPFT-2216
    		Inhibitor 99.35%
    FPFT-2216, a “molecular glue” compound, degrades phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3), and casein kinase 1α (CK1α). FPFT-2216 can be used for the research of cancer and inflammatory disease.
    FPFT-2216
Cat. No. Product Name / Synonyms Application Reactivity
Casein Kinase Isoform Comparison

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