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-N6841
    Rhodiolin
    		Inhibitor
    Rhodiolin, a flavonoid, is an orally active glucose 6-phosphate isomerase (GPI) inhibitor. Rhodiolin inhibits papillary thyroid cancer (PTC) by targeting glycolysis enzyme glucose 6-phosphate isomerase GPI and suppressing PI3K/AKT/mTOR phosphorylation and induce apoptosis. Rhodiolin as a NS2B-NS3 protease inhibitor can disrupt dengue viral replication. Rhodiolin is also a potential candidate for developing anticancer strategies inhibiting CK1ε kinase. Rhodiolin can be used for the study of anti-tumor and anti-viral .
    Rhodiolin
  • HY-50733A
    CX-5011
    		Inhibitor
    CX-5011 is a CK2 inhibitor. CX-5011 also induces Rac1 activation. CX-5011 induces apoptosis and induces cancer cell death.
    CX-5011
  • HY-160532
    CK1α degrader-1
    		Degrader
    CK1α degrader-1 (Compound 82) is an orally active CK1α degrader with a DC50 of 0.105 μM. CK1α degrader-1 can be used for the research of cancer.
    CK1α degrader-1
  • 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-50733
    CX-5011 free base
    		Inhibitor
    CX-5011 free base is a potent CK2 inhibitor. CX-5011 free base also is a Rac-1 activator. CX-5011 free base induces methuosis and promotes macropinocytosis. CX-5011 free base induces apoptosis. CX-5011 free base decreases the expression of rpS6 phosphorylation.
    CX-5011 free base
  • 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
  • HY-12470A
    PF-4800567 hydrochloride
    		Inhibitor
    PF-4800567 hydrochloride is a potent and selective inhibitor of?casein kinase?1? (CK1?), with an?IC50?of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM). PF-4800567 hydrochloride is useful in probing unique roles between these two kinases in multiple signaling pathways.
    PF-4800567 hydrochloride
  • HY-14393S
    Emodin-d4
    		Inhibitor
    Emodin-d4 is the deuterium labeled Emodin. 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-d<sub>4</sub>
  • HY-155958
    Casein kinase 1δ-IN-9
    		Inhibitor ≥98.0%
    Casein kinase 1δ-IN-9 (compound 737) is a potent casein kinase 1δ (CK1δ/CK15) inhibitor. Casein kinase 1δ-IN-9 can be used for the research of neurodegenerative disorders such as Alzheimer's disease.
    Casein kinase 1δ-IN-9
  • HY-117332
    IQA
    		Inhibitor
    IQA (CGP-029482) is a potent and selective protein kinase CK2 inhibitor.
    IQA
  • HY-P3748
    Casein Kinase II Receptor Peptide
    		Chemical
    Casein Kinase II Receptor Peptide is a substrate for casein kinase II with an Km value of 500 µM. Casein Kinase II Substrate can be used for measure casein kinase II activity in crude enzyme preparations.
    Casein Kinase II Receptor Peptide
  • HY-W011109
    CKI-7
    		Inhibitor
    CKI-7 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 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases.
    CKI-7
  • HY-170953
    QXG-6442
    		Inhibitor
    QXG-6442 is a CK1α Molecular Glue Degrader. QXG-6442 exhibits CK1α degradation potency with a DC50 of 5.7 nM and a Dmax of 90%. QXG-6442 induces antiproliferative effects in MOLM-14 cell line.
    QXG-6442
  • HY-169692
    Casein kinase 1δ-IN-21
    		Inhibitor
    Casein kinase 1δ-IN-21 (compound 501) is a potent casein kinase 1δ inhibitor. Casein kinase 1δ-IN-21 can be used in the study of neurodegenerative diseases such as Alzheimer's disease.
    Casein kinase 1δ-IN-21
  • HY-174350
    CK2-IN-15
    		Inhibitor
    CK2-IN-15 (Compound Biv5) is a selective and potent bivalent protein kinase CK2 inhibitor with an IC50 value of 51 pM. CK2-IN-15 significantly reduces the replication of SARS-CoV-2 in HEK-ACE2-TMPRSS2 and Vero cells, and also reduces viral replication in an ex vivo model of human nasal epithelial cells. CK2-IN-15 is promising for research of β-coronavirus infection-related diseases.
    CK2-IN-15
  • HY-171277
    Casein kinase 1δ-IN-27
    		Inhibitor
    Casein kinase 1δ-IN-27 (Compound 8) is the inhibitor for casein kinase 1 that inhibits CK1α, CK1δ, CK1ε, and p38α with IC50s of 22, 16.5, 9.41 and 14.8 nM, respectively. Casein kinase 1δ-IN-27 inhibits the DUX4 expression with an IC50 of 10 nM.
    Casein kinase 1δ-IN-27
  • HY-170859
    AH078
    		Inhibitor
    AH078 (compound 37) is a PROTAC degrader that selectively targets CK1δ and CK1ε, and has low targeting for CK1α. AH078 consists of PROTAC linker (black part) Monomethyl octanoate (HY-W001958), target protein ligand (red part) (HY-170860) CK1δ/CK1ε liagnd-1 and E3 ligase ligand (blue part) E3 ligase Ligand 58 (HY-170861). Among them, E3 ligase ligand + linker can form a conjugate E3 Ligase Ligand-linker Conjugate 163 (HY-170862).
    AH078
  • HY-169709
    Casein kinase 1δ-IN-26
    		Inhibitor
    Casein kinase 1δ-IN-26 (compound 505) is a potent casein kinase 1δ inhibitor. Casein kinase 1δ-IN-26 can be used in the study of neurodegenerative diseases such as Alzheimer's disease.
    Casein kinase 1δ-IN-26
  • HY-156913
    Casein kinase 1δ-IN-13
    		Inhibitor
    Casein kinase 1δ-IN-13 (compound 401) is a Casein kinase 1δ inhibitor. Casein kinase 1δ-IN-13 can be used in neurodegenerative disease research.
    Casein kinase 1δ-IN-13
Cat. No. Product Name / Synonyms Application Reactivity
Casein Kinase Isoform Comparison

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