2. Signaling Pathways
  3. Cell Cycle/DNA Damage
    Stem Cell/Wnt
  4. Casein Kinase
  5. CK1 Isoform

CK1

Casein kinase 1 (CK1) is a conserved family of serine/threonine protein kinases that includes the α, β, γ1-3, δ, and ε isoforms, which share highly conserved catalytic domains but differ in regulatory regions that influence substrate selection and cellular functions[1]. CK1 isoforms participate in multiple signaling networks and regulate protein phosphorylation events involved in cell survival, proliferation, differentiation, and intracellular signaling[1]. Mechanistically, CK1 has a central role in Wnt/β-catenin signaling, where distinct isoforms phosphorylate pathway components and control β-catenin stability and transcriptional activity[2]. In particular, CK1α functions as a negative regulator of canonical Wnt signaling by initiating phosphorylation events that promote β-catenin degradation and suppress pathway activation[2][3]. Dysregulation of CK1-dependent signaling has been linked to tumorigenesis and other disease processes, making CK1 an important experimental target in cancer biology and signal transduction research[1][2]. Compared with related isoforms, CK1α shows a prominent role in restraining Wnt signaling, whereas CK1δ and CK1ε are strongly associated with circadian clock regulation through phosphorylation-dependent control of PERIOD protein stability and localization[1][4][5]. In disease and physiological models, alterations in CK1δ or CK1ε activity have been associated with circadian rhythm disorders, while aberrant CK1 signaling has also been implicated in neurodegenerative pathology[4][5]. For experimental applications, small-molecule CK1 modulators, including isoform-targeting inhibitors such as IC261, have been used to investigate CK1-dependent signaling mechanisms and disease-relevant pathways[1].

CK1 Related Products (74):

Cat. No. Product Name Effect Purity
  • 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.
  • HY-148251
    MU1742
    		99.54%
    MU1742 is a probe for CK1δ and CK1ε protein kinases.
  • 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.
  • 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.
  • HY-W011109
    CKI-7
    		Inhibitor 99.97%
    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.
  • HY-170859
    AH078
    		Inhibitor 99.73%
    AH078 is a PROTAC-based CK1δ/ε degrader (DC50=0.55 μM, Dmax=70%) that lacks subtype selectivity between CK1δ and CK1ε. AH078 induces target protein degradation either by recruiting the CUL4-CRBN E3 ligase complex and proteasome, or via the VHL- and ubiquitin-dependent pathway. AH078 also exhibits selectivity for CK1α, and is widely applicable to research related to colon cancer, pancreatic cancer, breast cancer, ovarian cancer, chronic lymphocytic leukemia, acute myeloid leukemia, glioma, and metastatic breast adenocarcinoma.
  • HY-15704
    LH846
    		Inhibitor 98.89%
    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.
  • 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.
  • HY-N6841
    Rhodiolin
    		Inhibitor 98%
    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 .
  • 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.
  • HY-168615
    MGD-28
    		Degrader 99.73%
    MGD-28 is a potent, orally active, Cereblon (CRBN)-dependent IKAROS protein degrader that degrades IKZF1 (DC50=3.8 nM), IKZF2 (DC50=56.3 nM), and IKZF3 (DC50=7.1 nM) in a dose-dependent manner. In addition, MGD-4 also degrades CK1α (DC50=7.8 nM). MGD-28 has antiproliferative activity and can be used in multiple myeloma research.
  • HY-170953
    QXG-6442
    		Inhibitor 99.52%
    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.
  • HY-148455
    Casein kinase 1δ-IN-3
    		Inhibitor 99.50%
    Casein kinase 1δ-IN-3 (Compound 23a) is a casein kinase 1 delta (CK1d) inhibitor with a pIC50 of 6.5376 M.
  • HY-137340
    WH-10417-099
    		Degrader 98.14%
    WH-10417-099 is a CRBN-based PROTAC multi-kinase degrader that induces the degradation of the maximum number of unique kinases (over 125 unique kinases, such as CSNK1E and PI3Kγ) simultaneously. WH-10417-099 induces protein degradation via the ubiquitin biotinylation (E-STUB) pathway, exhibits synergistic effects with SB-405483 (HY-W1135319). The E3 ligase ligand and linker of WH-10417-099 can form the conjugate Pomalidomide 4'-PEG5-acid (HY-131647).
  • HY-117857
    MRT00033659
    		Inhibitor 99.77%
    MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC50=0.9 μM for CK1δ) and CHK1 (IC50=0.23 μM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation.
  • HY-103383
    (R)-DRF053 dihydrochloride
    		Inhibitor 99.30%
    (R)-DRF053 dihydrochloride is a potent casein kinases 1 (CK1), CDK1/cyclin B and CDK5/p25 inhibitor with IC50s of 14 nM, 220 nM and 80 nM, respectively. (R)-DRF053 dihydrochloride prevents the CK1-dependent production of amyloid-beta in a cell model.
  • HY-148112
    Casein kinase 1δ-IN-1
    		Inhibitor 99.91%
    Casein kinase 1δ-IN-1 is an inhibitor of casein kinase 1δ (CK1δ). Casein kinase 1δ-IN-1 can be used for the research of neurodegenerative diseases such as tauopathies.
  • HY-128677
    NCC007
    		Inhibitor 99.22%
    NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor with IC50s of 1.8 and 3.6 μM, respectively. NCC007 can be used in research of modulating mammalian circadian rhythms.
  • HY-108907
    SR-1277
    		Inhibitor 99.51%
    SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer.
  • HY-125957
    A-3 hydrochloride
    		Inhibitor 99.75%
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
Cat. No. Product Name / Synonyms Application Reactivity