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-168517
    PIM-1/CK2-IN-2
    		Inhibitor
    PIM-1/CK2-IN-2 (compound 3aA) is a PIM-1/CK2 inhibitor. PIM-1/CK2-IN-2 can induce the mitochondrial apoptotic pathway in CCRF-CEM cells. PIM-1/CK2-IN-2 can be used in cancer research.
    PIM-1/CK2-IN-2
  • HY-156040
    Casein kinase 1δ-IN-10
    		Inhibitor
    Casein kinase 1δ-IN-10 is a casein kinase 1δ (CK1δ) inhibitor (WO2012080729A2; compound 685).
    Casein kinase 1δ-IN-10
  • HY-120267
    TID43
    		Inhibitor
    TID43 is a CK2 inhibitor, with an IC50 of 0.3 μM. TID43 can be used for anti-angiogenic research.
    TID43
  • HY-128433
    CK1-IN-3
    		Inhibitor 99.00%
    CK1-IN-3 (compound 51) is a AC1 inhibitor with an IC50s 2.22 µM for CK-1δ.
    CK1-IN-3
  • HY-158370
    CK2-IN-11
    		Inhibitor
    CK2-IN-11 (32) is an allosteric CK2 inhibitor, with high selectivity for CK2 with IC50 values of 19.3 nM and 15.6 nM for the CK2α2β2 and the CK2α′2β2 isoforms, respectively.
    CK2-IN-11
  • HY-182800
    IBA-11
    		Degrader
    IBA-11 is a selective CRBN-dependented CK1α molecular glue degrader. IBA-11 binds to the canonical tri-tryptophan pocket of CRBN, forming a ternary complex with CK1α to mediate its degradation. IBA-11 induces CRBN-dependent ubiquitin-proteasome system-mediated degradation of CK1α. IBA-11 exhibits cytotoxicity against cancer cells. IBA-11 demonstrates in vitro metabolic stability in rat liver microsomes and minimal hERG inhibition. IBA-11 can be used for the research of cancer, such as acute myeloid leukemia.
    IBA-11
  • HY-170859A
    AH081
    		Inhibitor
    AH081 (Compound 38) is a CK1δ/ε PROTAC degrader. AH081 is the negative control compound of AH078 (HY-170859). AH081 has inhibitory but no degradation activity for CK1δ/ε by using an inactive stereoisomer of the VHL ligand. Pink: CK1δ/ε ligand (HY-148251); Blue: VHL ligase ligand (HY-125845B); Black: linker
    AH081
  • HY-135816
    CK2/PIM1-IN-1
    		Inhibitor
    CK2/PIM1-IN-1 is an inhibitor of CK2 and PIM1, with IC50s of 3.787 μM and 4.327 μM for CK2 and PIM1, respectively. CK2/PIM1-IN-1 is developed for the research of proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders.
    CK2/PIM1-IN-1
  • HY-162756
    CK1-IN-4
    		Inhibitor
    CK1-IN-4 (Compound 59) is an inhibitor for casein kinase CK1δ with IC50 of 2.74 μM. CK1-IN-4 exhibits neuroprotective effect in Ethacrynic acid (HY-B1640)-treated SH-SY5Y cells.
    CK1-IN-4
  • HY-49459
    Casein kinase 1δ-IN-14
    		Inhibitor
    Casein kinase 1δ-IN-14 (compound 481) is a casein kinase inhibitor that can be used to study neurodegenerative diseases such as Alzheimer's disease.
    Casein kinase 1δ-IN-14
  • HY-169573
    Casein kinase 1δ-IN-16
    		Inhibitor
    Casein kinase 1δ-IN-16 (compound 506) is a casein kinase 1δ (CK1δ) inhibitor. Casein kinase 1δ-IN-16 can be utilized in neurodegenerative disorders research.
    Casein kinase 1δ-IN-16
  • HY-135629
    PF-5236216
    		Inhibitor
    PF-5236216 is a brain-penetrant CK1δ/CK1ε inhibitor with IC50 values of 8 and 36 nM. PF-5236216 inhibits CK1δ and CK1ε-mediated PER3 nuclear translocation. PF-5236216 forms an H-bond with the backbone NH of Leu85, hydrophobic stacking with Met82, and a water-mediated H-bond with Lys38 of CK1δ. PF-5236216 can be used as a tool ligand for CNS PET studies.
    PF-5236216
  • HY-174347
    Hsp90-Cdc37-IN-4
    		Inhibitor
    Hsp90-Cdc37-IN-4, a Celastrol (HY-13067) derivative, inhibits the Hsp90-Cdc37 protein-protein interaction (PPI). Hsp90-Cdc37-IN-4 selectively inhibits casein kinase 2 (CK2), reducing phosphorylation of its substrate Cdc37 at Serine 13. Hsp90-Cdc37-IN-4 induces G0/G1 cell cycle arrest and triggers apoptosis via the mitochondrial pathway. Hsp90-Cdc37-IN-4 demonstrates potent anti-breast cancer activity.
    Hsp90-Cdc37-IN-4
  • HY-181022
    BMS-135
    		Inhibitor
    BMS-135 is a potenr, selective and ATP-competitive casein kinase 2 (CK2) inhibitor with IC50 of 0.8 and 0.3 nM for CK2αandCK2α′ isoforms. BMS-135 can simulate the structure of ATP and bind to the active pocket of CK2, thereby inhibiting its serine/threonine phosphorylation function. BMS-135 can inhibit cells proliferation and shows anti-tumor effect. BMS-135 can be used for research of colon cancer.
    BMS-135
  • HY-P3921
    Casein Kinase II Substrate
    Casein Kinase II Substrate is a casein kinase II (CK2) peptide substrate that can be selectively phosphorylated by CK2.
    Casein Kinase II Substrate
  • HY-164578
    CK1δ-IN-1
    		Inhibitor
    CK1δ-IN-1 (example 939) is a casein kinase 1 delta (CK1δ) inhibitor. CK1δ-IN-1 can be used for the study of Alzheimer's disease.
    CK1δ-IN-1
  • HY-121792
    CK2-IN-1
    		Inhibitor
    CK2-IN-1 is a CK2 inhibitor, with an IC50 of 150 nM.
    CK2-IN-1
  • HY-181586
    CK1γ-IN-1
    		Inhibitor
    CK1γ-IN-1 is a non-selective CK1 kinase inhibitor with IC50 values of 780 nM, 570 nM and 990 nM against human CK1γ1, CK1γ2, CK1γ3, respectively. The non-specific binding of CK1γ-IN-1 to multiple kinases enables its application in biological studies of specific CK1γ.
    CK1γ-IN-1
  • HY-108642A
    AMG-548 hydrochloride
    		Inhibitor
    AMG-548 hydrochloride, 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 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
    AMG-548 hydrochloride
  • HY-181442
    CK2-TN03
    		Inhibitor 98.02%
    CK2-TN03 is an ATP-competitive casein kinase 2 (CK2) inhibitor, with an IC50 of 165 nM and a Ki of 20 nM. CK2-TN03 inhibits CK2-mediated survivin activation and reduces CK2-dependent phosphorylation levels of BRD4/MYCN and AKT1. CK2-TN03 exerts anti-neuroblastoma effects by inhibiting survivin, leading to mitotic catastrophe and apoptosis of cancer cells. CK2-TN03 can be used in studies related to neuroblastoma.
    CK2-TN03
Cat. No. Product Name / Synonyms Application Reactivity
Casein Kinase Isoform Comparison

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