Casein kinase 1δ-IN-9 is a Quinone reductase 2 inhibitor with IC50 of 0.6μM.

Casein kinase 1δ-IN-8 is an inhibitor of casein kinase 1δ and is used to treat neurodegenerative diseases such as Alzheimer's disease type.

Casein kinase 1δ-IN-4 (compound 567) is a potent inhibitor of casein kinase 1δ with potential application in Alzheimer's disease research [1].

Casein kinase 1δ-IN-3 (Casein kinase 1δ-IN-3) (Compound 23a) is a casein kinase 1 delta (CK1d) inhibitor with a pIC50 of 6.5376 M.

Casein kinase 1δ-IN-5 is a potent and selective CK-1δ inhibitor, exhibiting an IC50 of 47 nM, and demonstrates neuroprotective and anti-inflammatory effects in vitro, with potential applications in neurodegenerative disease research.

Casein kinase 1δ-IN-7 is a Casein kinase 1δ inhibitor for neurodegenerative diseases such as Alzheimer's disease.

Casein kinase 1δ-IN-10 is an inhibitor of casein kinase 1δ (CK1δ).

Casein kinase 1δ-IN-6 is a potent and selective inhibitor of the protein kinase CK-1δ with an IC50 of 23 nM.Casein kinase 1δ-IN-6 shows neuroprotective and anti-inflammatory activity in both in vitro and in vivo assays.Casein kinase 1δ-IN-6 can be used to study neurodegenerative diseases.

CK2/ERK8-IN-1 (TMCB) is a dual inhibitor of casein kinase 2 (CK2) (Ki: 0.25 µM) and ERK8 (IC50s: 0.50 μM) with pro-apoptotic efficacy. CK2/ERK8-IN-1 also binds to PIM1, DYRK1A, and HIPK2 (Kis: 8.65 µM, 11.9 µM, and 15.25 µM).

Casein Kinase 2 Substrate Peptide, a widely recognized CK2 substrate, is synthesized with its C-terminus conjugated to 5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid (EDANS). This peptide serves as a tool for determining protein kinase CK2 activity [1].

QLT0267 is an inhibitor targeting integrin-linked kinase (ILK; IC50= 26 nM), showing over 10-fold selectivity against cyclin-dependent kinases 1, 2, and 5 (Cdk1, Cdk2, and Cdk5), and over 1,000-fold selectivity against C-terminal Src kinase (CSK), DNA-PK, Pim-1, Akt, PKC, and casein kinase 2 (CK2) at a concentration of 10 mg/ml. This compound effectively inhibits the proliferation of NPA187 papillary thyroid cancer cells with an IC50 of approximately 3 µM and induces apoptosis in NPA187, DRO, and K4 cancer cell lines. In vivo studies reveal that QLT0267, administered at 100 mg/kg, significantly reduces tumor growth in a DRO mouse xenograft model and diminishes both tumor volume and intratumoral vascularization in a U87MG glioblastoma mouse xenograft model, showcasing its potential for therapeutic applications in cancer treatment.

CK1-IN-1 (PUN51207) is a casein kinase 1 (CK1) inhibitor. CK1-IN-1 has IC50s of 15 nM, 16 nM, 73 nM for CK1δ, and CK1ε, p38σ MAPK, respectively.

PF-05236216 hydrochloride is a brain penetrant, potent and selective inhibitor of casein kinase 1 delta/epsilon (CK1δ/ε) that modulates circadian rhythms in mice.

TMX-4113 has potential to be used in cancer that is a phosphodiesterase 6D(PDE6D) and casein kinase 1α(CK1α) degrader [1].

Casein Kinase II Substrate, a peptide substrate, is selectively phosphorylated by casein kinase II (CK2) [1].

TMX-4116, a casein kinase 1α (CK1α) degrader, preferentially degrades CK1α in MOLT4, Jurkat, and MM.1S cells, exhibiting degradation concentration 50s (DC50s) below 200 nM. TMX-4116 is utilized in the research of multiple myeloma [1].

AMG-548 dihydrochloride is a selective, orally active p38α inhibitor with a Ki value of 0.5 nM, a slight selectivity for p38β (Ki=36 nM) and >1000-fold selectivity for p38γ and p38δ. AMG-548 dihydrochloride exhibits inhibition of whole blood LPS-stimulated TNFα with an IC50 value of 3 nM. AMG-548 dihydrochloride directly inhibited casein kinase 1 isoforms δ and ε, and inhibited Wnt signaling.

Epiblastin A is an inhibitor of Casein Kinase 1 (CK1). Epiblastin A engages CK1 isoenzymes in cell lysate and induces efficient conversion of epiblast stem cells (EpiSCs) into embryonic stem cells (cESCs).

AMG-548 hydrochloride is a selective, orally active p38α inhibitor with a Ki value of 0.5 nM, a slight selectivity for p38β (Ki=36 nM) and a 1000-fold selectivity for p38γ and p38δ. AMG 548 hydrochloride also effectively inhibits whole blood LPS-stimulated TNFα with an IC50 value of 3 nM. AMG-548 hydrochloride directly inhibited casein kinase 1 isoforms δ and ε, which in turn inhibited Wnt signaling.

A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively[1]. A-3 hydrochloride against P

CKI-7 free base is a potent and ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.

ON 108600 is a chemical inhibitor targeting CK2 (Casein Kinase 2), TNIK, and DYRK1, demonstrating IC50 values of 0.016 μM and 0.007 μM for DYRK1A and DYRK1B, 0.028 μM for DYRK2, 0.05 μM and 0.005 μM for CK2α1 and CK2α2, and 0.005 μM for TNIK, respectively. This compound exhibits antitumor activity [1].

D4476 (Casein Kinase I Inhibitor) is an effective, selective, and cell-permeant CK1 (casein kinase 1) inhibitor( IC50=300 nM in a cell-free assay).

Umbralisib (TGR-1202) sulfate, an orally active compound, serves as a potent, selective inhibitor targeting both PI3Kδ and casein kinase-1-ε (CK1ε), with EC50 values of 22.2 nM and 6.0 μM, respectively. It demonstrates unique immunomodulatory effects on T cells in chronic lymphocytic leukemia (CLL) and is applicable in the research of hematological malignancies.

Umbralisib Tosylate (TGR-1202) is a potent, selectively dual inhibitor targeting PI3Kδ and casein kinase-1-ε (CK1ε), demonstrating oral activity. With EC50 values of 22.2 nM and 6.0 μM for PI3Kδ and CK1ε respectively, it shows unique immunomodulatory effects on T cells in chronic lymphocytic leukemia (CLL). This compound is utilized in the research of hematological malignancies.

Myelin Basic Protein (MHP4-14) TFA, a synthetic peptide containing residues 4-14 of myelin basic protein, serves as a highly selective substrate for protein kinase C (PKC) with a K_m of 7 μM. It is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca^2+/calmodulin-dependent protein kinase II, or phosphorylase kinase. This specificity makes Myelin Basic Protein TFA an ideal candidate for protein kinase C assays in crude tissue extracts, ensuring minimal background interference [1] [2].

Casein Kinase II Receptor Peptide, a substrate for casein kinase II, exhibits a Km value of 500 µM. It is utilized to measure the activity of casein kinase II in crude enzyme preparations [1].

CKI-7 is a potent and ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.