1. Signaling Pathways
  2. Cell Cycle/DNA Damage
    Stem Cell/Wnt
  3. Casein Kinase

Casein Kinase

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-176561
    IOR-160
    Inhibitor
    IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDACs. IOR-160 exhibits high selectivity for CK2 (IC50 = 1.7 nM) and broad inhibitory activity against HDAC (HDAC 1, 2, 3, and 6 with IC50s of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, with low activity for HDAC8). IOR-160 modulates key cellular signaling pathways by inhibiting AKT phosphorylation and increasing acetylated α-tubulin. IOR-160 inhibits tumor growth and reduces tumor burden through dual CK2/HDAC inhibition. IOR-160 is indicated for use in triple-negative breast cancer research.
    IOR-160
  • HY-W842364
    CK1δ-IN-3
    Inhibitor
    CK1δ-IN-3 (compound 376) is a casein kinase 1δ (CK1δ) inhibitor. CK1δ-IN-3 can be utilized in neurodegenerative disorders research.
    CK1δ-IN-3
  • HY-169706
    Casein kinase 1δ-IN-25
    Inhibitor
    Casein kinase 1δ-IN-25 (compound 487) is a potent casein kinase 1δ inhibitor. Casein kinase 1δ-IN-25 can be used in the study of neurodegenerative diseases such as Alzheimer's disease.
    Casein kinase 1δ-IN-25
  • HY-169629
    CK2 inhibitor 4
    Inhibitor
    CK2 inhibitor 4 (compound 5b) is a protein kinase CK2 inhibitor with IC50 of 3.8 μM. CK2 inhibitor 4 can be used in tumor research.
    CK2 inhibitor 4
  • HY-176825
    MU1742-amide-C6-acid
    Inhibitor
    MU1742-amide-C6-acid is a CK1δ/ε inhibitor. MU1742-amide-C6-acid can be used for synthesis of PROTAC AH081 (HY-170859A).
    MU1742-amide-C6-acid
  • HY-171278
    Casein kinase 1δ-IN-28
    Inhibitor
    Casein kinase 1δ-IN-28 (Compound 4) is the inhibitor for CK1ε with an IC50 of 0.0146 μM. Casein kinase 1δ-IN-28 exhibits a metabolite rate in human liver microsomes of 52%.
    Casein kinase 1δ-IN-28
  • HY-112477A
    (E/Z)-Chk2-IN-1
    Inhibitor
    (E/Z)-Chk2-IN-1 ((E/Z)-Hymenialdisine analogue-1) (Compound 1) is a potent and selective cell cycle kinase Chk2 inhibitor with an IC50 of 8 nM. (E/Z)-Chk2-IN-1 exhibits low inhibitory activity against other kinases (such as CK1δ, MEK1, and PKCα/βⅡ) with IC50 values both >89 nM. (E/Z)-Chk2-IN-1 can be used for the research of cancer.
    (E/Z)-Chk2-IN-1
  • HY-181048
    CK1α-IN-1
    Inhibitor
    CK1α-IN-1 (Compound 7a) is a selective CK1α inhibitor with an IC50 of 10.96 nM. CK1α-IN-1 dose-dependently stabilizes p53 protein. CK1α-IN-1 has anticancer activity against acute monocytic leukemia.
    CK1α-IN-1
  • HY-146138
    EGFR-IN-57
    Inhibitor
    EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis.
    EGFR-IN-57
  • HY-162336
    Casein kinase 1δ-IN-15
    Inhibitor
    Casein kinase 1δ-IN-15 is an inhibitor for casein kinase 1 (CK1δ), with an IC50 of 0.045 μM.
    Casein kinase 1δ-IN-15
  • HY-123859
    SR-2890
    Inhibitor
    SR-2890 is a highly selective, ATP-competitive inhibitor of casein kinase CK1δ and CK1ε, with IC50 values ​​of 4 nM and 44 nM, respectively, and a Ki of 14 nM for CK1δ. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase activity of CK1δ and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of <1%. SR-2890 demonstrates stable in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1δ/ε-related diseases such as Alzheimer's disease.
    SR-2890
  • HY-163182
    CSNK2A-IN-2
    Inhibitor
    CSNK2A-IN-2 (compound 6c) is a selective CSNK2A inhibitor with antiviral activity. CSNK2A-IN-2 exhibits an inhibitory effect on viral replication and is selective for PIM3.
    CSNK2A-IN-2
  • HY-P11119
    CKS peptide
    CKS peptide is a selective substrate peptide for CK1. CKS peptide can used to measure CK1 activity.
    CKS peptide
  • HY-B1035A
    Levobunolol
    Inhibitor
    Levobunolol (l-Bunolol) is a non-selective β-adrenergic antagonist and vasodilator. By blocking calcium ion influx and reducing the sensitivity of vascular smooth muscle to calcium, Levobunolol effectively dilates the ciliary arteries and increases ocular blood flow, so it is widely used in research on glaucoma and ocular hypertension. Levobunolol inhibits the β-receptor signaling pathway and the expression of related proliferation markers (such as CK3, CK14, CK19, Ki67) in corneal cells. In rabbit models, Levobunolol not only does not inhibit corneal epithelial regeneration, but also accelerates the healing of mechanical injury without adverse effects. Levobunolol also inhibits histamine-induced vasoconstriction and intracellular calcium elevation, exhibiting unique vascular regulatory activity. Levobunolol protects ocular blood flow and promotes corneal repair.
    Levobunolol
  • HY-105222A
    CHX-3107
    Inhibitor
    CHX-3107 is a casein kinase 2 inhibitor .
    CHX-3107
  • HY-P1909
    Casein Kinase Substrates 3
    Casein Kinase Substrates 3 is a substrate of casein kinase.
    Casein Kinase Substrates 3
  • HY-169689
    Casein kinase 1δ-IN-19
    Inhibitor
    Casein kinase 1δ-IN-19 (compound 492) is a potent casein kinase 1δ inhibitor. Casein kinase 1δ-IN-19 can be used in the study of neurodegenerative diseases such as Alzheimer's disease.
    Casein kinase 1δ-IN-19
  • HY-P5526
    CCK1-specific peptide substrate
    CCK1-specific peptide substrate is a biological active peptide. (This peptide sequence is based on rabbit muscle glycogen synthase with Ser7 phosphorylated. It is a peptide substrate for Casein Kinase I (CK1). CK1 phosphorylates Ser10. Ser7 is phosphorylated by PKA in vivo.)
    CCK1-specific peptide substrate
  • HY-169668
    WAY-606344
    Inhibitor
    WAY-606344 (Compound 97) is a Casein kinase 1δ inhibitor. WAY-606344 is promising for research of Alzheimer's disease.
    WAY-606344
  • HY-175600
    MI-2-80
    Degrader
    MI-2-80 is a molecular glue degrader. MI-2-80 induces proteins (such as IKZF1/3 and CSNK1A1) to bind to CRBN, promoting their ubiquitination and degradation.
    MI-2-80
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