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-10108R
    LY294002 (Standard)
    		Inhibitor
    LY294002 (Standard) is the analytical standard of LY294002. This product is intended for research and analytical applications. 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 (Standard)
  • 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-100011R
    SR-3029 (Standard)
    		Inhibitor
    SR-3029 (Standard) is the analytical standard of SR-3029 (HY-100011). This product is intended for research and analytical applications. 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 (Standard)
  • HY-B0183R
    Ellagic acid (Standard)
    		Inhibitor
    Ellagic acid (Standard) is the analytical standard of Ellagic acid. This product is intended for research and analytical applications. 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 (Standard)
  • 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-178980
    APL-5125
    		Inhibitor
    APL-5125 (Compound 61f) is a potent, selective and orally active ATP-competitive CK2α inhibitor with an IC50 of 0.348 nM and a Ki of 0.095 nM. APL-5125 binds to CK2α in a bivalent manner, simultaneously interacting with the ATP-binding site and the αD pocket. APL-5125 exhibits antitumor activity and can be used for the research of cancer, such as colon cancer.
    APL-5125
  • HY-174458
    MD-4251
    MD-4251 is an orally active MDM2 PROTAC degrader. MD-4251 potently degrades MDM2 in RS4;11 cells (DC50: 0.2 nM) and actives p53. MD-4251 shows strong antiproliferative activity against acute leukemia cells (wild-type p53) with minimal efficacy in mutant type. MD-4251 induces complete tumor regression in RS4;11 xenograft mice model. Pink: MDM2 ligand (HY-130684); Blue: CRBN ligase ligand (HY-W883326); Black: linker
    MD-4251
  • 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-169690
    Casein kinase 1δ-IN-20
    		Inhibitor
    Casein kinase 1δ-IN-20 (compound 427) is a potent casein kinase 1δ inhibitor. Casein kinase 1δ-IN-20 can be used in the study of neurodegenerative diseases such as Alzheimer's disease.
    Casein kinase 1δ-IN-20
  • 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-171298
    CK1δ-IN-10
    		Inhibitor
    CK1δ-IN-10 (Compound 85) is the inhibitor for casein kinase 1 that inhibits CK1δ (CSNKID) with IC50 of 0.255 μM.
    CK1δ-IN-10
  • 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-P11496
    CK2 Substrate peptide
    		Substrate
    CK2 Substrate peptide (Compound RRRADDSDDDDD) is a specific CK2 peptide substrate with Km of 13 μM. CK2 Substrate peptide can be used for the research of neurological disease, such as Alzheimer's Disease.
    CK2 Substrate peptide
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Casein Kinase Isoform Comparison

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