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-120084
    BTX161
    		Inhibitor 99.20%
    BTX161, a thalidomide analog, is an effective CKIα degrader. BTX161 mediates human AML cell CKIα degradation more effectively than lenalidomide and activates the DNA damage response (DDR) and p53, while stabilizing p53 antagonist MDM2.
    BTX161
  • HY-148491
    CSNK1-IN-2
    		Inhibitor 99.22%
    CSNK1-IN-2 is a CSNK1A1 inhibitor. CSNK1-IN-1 has inhibitory activity for CSNK1A1 kinase with IC50 values of 2.52 μM. CSNK1-IN-2 can be used for the research of proliferative disorders.
    CSNK1-IN-2
  • HY-158975
    VRK1/CK1-IN-1
    		Inhibitor 98.69%
    VRK1/CK1-IN-1 (compound 36) is a dual inhibitor of vaccinia-related kinase 1 (VRK1) and casein kinase 1 (CK1), with the Ki of 37.9 nM for VRK1 and IC50s of 17 nM and 15 nM for δ and ε isoforms of CK1, respectively.
    VRK1/CK1-IN-1
  • HY-153866
    CK1-IN-2
    		Inhibitor 99.54%
    CK1-IN-2 (compound Nr.4) is a potent CK1 inhibitor with an IC50 values of 123, 19.8, 26.8, 74.3 nM for CK1a, CK1d, CK1e, p38a, respectively.
    CK1-IN-2
  • HY-114858
    Epiblastin A
    		Inhibitor 99.51%
    Epiblastin A is an ATP competitive casein kinase 1 (CK1) inhibitor with IC50s of 8.9, 0.5, and 4.7 µM for CK1α, CK1δ, and CK1 ɛ, respectively. Epiblastin A induces reprogramming of epiblast stem cells into embryonic stem cells by inhibition of CK1.
    Epiblastin A
  • HY-108606
    PI-828
    		Inhibitor 99.62%
    PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively.
    PI-828
  • HY-P3815
    Casein Kinase 2 Substrate Peptide
    		98.47%
    Casein Kinase 2 Substrate Peptide is a common CK2 substrate peptide. Casein Kinase 2 Substrate Peptide is synthesized with its C-terminus conjugated to 5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid (EDANS). Casein Kinase 2 Substrate Peptide can be used for protein kinase CK2 activity determination.
    Casein Kinase 2 Substrate Peptide
  • HY-100114
    TA-01
    		Inhibitor 99.86%
    TA-01 is a potent CK1 and p38 MAPK inhibitor, with IC50s of 6.4 nM, 6.8 nM, 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively. TA-01 acts as a cardiogenic inhibitor.
    TA-01
  • HY-132175
    CK2 inhibitor 2
    		Inhibitor 98.51%
    CK2 inhibitor 2 is a potent, selective and orally active inhibitor of CK2, with an IC50 of 0.66 nM. CK2 inhibitor 2 shows high selectivity for Clk2 (IC50=32.69 nM)/CK2. CK2 inhibitor 2 exhibits favorable antiproliferative and antitumor activity.
    CK2 inhibitor 2
  • HY-111820
    CK1-IN-1
    		Inhibitor 99.19%
    CK1-IN-1 (Compound 1c) is a casein kinase 1 (CK1) inhibitor with IC50 values of 15 nM and 16 nM for CK1δ and CK1ε, respectively. CK1-IN-1 inhibits p38α MAPK with an IC50 of 73 nM. CK1-IN-1 can be used to study cardiomyogenesis.
    CK1-IN-1
  • HY-110052
    TBCA
    		Inhibitor 99.45%
    TBCA is a highly selective CK2 (casein kinase II) inhibitor with an IC50 of 110 nM and a Ki of 77 nM. TBCA shows selectivity for CK2 over CK1, DYRK1A and a panel of 27 other kinases.
    TBCA
  • HY-156816
    ON 108600
    		Inhibitor 99.73%
    ON 108600 is a inhibitor for CK2 (Casein Kinase2)/TNIK/DYRK1 , with the IC50s for DYRK1A/DYRKB, DYRK2, CK2α1/CK2α2, and TNIK of 0.016 μm/0.007 μM, 0.028 μM, 0.05 μM/0.005 μM, and 0.005 μM, respectively. ON 108600 has antitumor activity.
    ON 108600
  • HY-18285
    Longdaysin
    		Inhibitor 99.83%
    Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of  5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively.
    Longdaysin
  • HY-123955
    Casein Kinase inhibitor A86
    		Inhibitor 99.26%
    Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb). Casein Kinase inhibitor A861 induces leukemia cell apoptosis, and has potent anti-leukemic activities.
    Casein Kinase inhibitor A86
  • HY-15704
    LH846
    		Inhibitor 98.18%
    LH846 is a selective inhibitor of CKIδ, with an IC50 of 290 nM, and less potently inhibits CKIα and CKIε, with IC50s of 2.5 μM and 1.3 μM, respectively.
    LH846
  • HY-145320
    TMX-4113
    		Inhibitor 99.08%
    TMX-4113 is a degrader of phosphodiesterase 6D (PDE6D) and casein kinase 1α (CK1α). TMX-4113 can be used for the research of cancer.
    TMX-4113
  • HY-108642
    AMG-548
    		Inhibitor ≥99.0%
    AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
    AMG-548
  • HY-N3127
    Orobol
    		Inhibitor 99.28%
    Orobol is one of the major soy isoflavones and has various pharmacological activities, including anti-skin-aging and anti-obesity effects. Orobol inhibits CK1ε, VEGFR2, MAP4K5, MNK1, MUSK, TOPK, and TNIK (IC50=1.24-4.45 μM). Orobol also inhibits PI3K isoforms (IC50=3.46-5.27 μM for PI3K α/β/γ/K/δ).
    Orobol
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
Casein Kinase Isoform Comparison

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