Casein Kinase

Casein kinase 1δ-IN-5 is a selective CK1δ inhibitor (IC50 47 nM) with neuroprotective activity, supporting neurodegeneration research.

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

PF-05236216 is a potent, selective, brain-penetrant CK1δ/ε inhibitor that modulates circadian rhythms in mice, supporting sleep and metabolic research.

Casein Kinase II Inhibitor IV HCl promotes keratinocyte differentiation, potential for skin disorder therapy.

CK2-IN-3: potent, selective CK2 inhibitor; Kd=12 nM, IC50: 1.51 μM (CK2α), 7.64 μM (CK2α'). For cancer research.

Casein kinase1δ-IN-13 (compound 401) is an inhibitor of Casein kinase1δ. It is utilized in the research of neurodegenerative diseases.

Casein kinase1δ-IN-23 (compound 423) is an effective inhibitor of casein kinase1δ. It is applicable in research related to neurodegenerative diseases such as Alzheimer's disease.

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

Casein kinase1δ-IN-17 (compound 753) is an inhibitor of casein kinase 1δ (CK1δ). It is applicable in research related to neurodegenerative diseases.

Casein kinase1δ-IN-28 (Compound 4) is an inhibitor of CK1ε, with an IC50 of 0.0146 μM. The human liver microsome metabolism rate for Casein kinase1δ-IN-28 is 52%.

CK1δ-IN-6 (Compound 303) is an inhibitor of Casein kinase 1δ, with potential applications in Alzheimer's disease research.

WAY-606344 (Compound 97) is an inhibitor of Casein kinase 1δ and shows potential for Alzheimer's disease research.

CK1δ-IN-5 (Compound 24) is an inhibitor of casein kinase 1δ (CK1δ) and can be used in the study of neurodegenerative diseases.

Casein kinase1δ-IN-27 (Compound 8) is an inhibitor of casein kinase 1 (CK1), effectively inhibiting CK1α, CK1δ, CK1ε, and p38α with IC50 values of 22, 16.5, 9.41, and 14.8 nM, respectively. It also suppresses DUX4 expression, with an IC50 of 10 nM.

CK1δ-IN-7 (Compound 488) is an inhibitor of casein kinase 1δ (CK1δ).

(R,R)-BMS-986397 is a CK1α degrader with a DC50 ranging from 0.1 to 0.5 pM. This compound is applicable in leukemia research.

dCK1α-2 is an orally effective CK1α molecular glue (Molecular Glue) degrader that targets p53 pathway-related targets. It demonstrates antitumor efficacy in mouse models by enhancing the expression of p53-related genes.

p38α inhibitor8 (Compound 1) demonstrates inhibitory activity against p38αMAPK and CK1δ, with IC50 values of 0.21 µM and 0.202 µM, respectively.

CK1δ-IN-9 (Compound 8) is an inhibitor of casein kinase 1 (CK1), specifically targeting CK1δ with an IC50 of 1.4 nM. The compound also inhibits p38α and p38β with IC50 values of 0.25 μM and 0.78 μM, respectively. CK1δ-IN-9 exhibits favorable pharmacokinetic properties, including high oral bioavailability (70%) and moderate clearance.

MGD-28 is a Cullin-CRBN-dependent IKZF family protein degrader for IKZF1 (Ikaros), IKZF2 (Helios), IKZF3 (Aiolos) ,and CK1α, antiproliferative.

Casein kinase1δ-IN-31 (Compound 16) is an inhibitor of casein kinase (CK), specifically targeting CK1α, CK1δ, and p38α, with IC50 values of 196 nM, 17 nM, and 18 nM, respectively. Additionally, Casein kinase1δ-IN-31 inhibits Double Homeobox 4 (DUX4) with an IC50 of 1200 nM.

CK1δ-IN-10 (Compound 85) is an inhibitor of casein kinase 1 (CK1), specifically targeting CK1δ (CSNKID), with an IC50 value of 0.255 μM.

Casein kinase1δ-IN-16 (compound 506) is an inhibitor of casein kinase 1δ (CK1δ). This compound is applicable in research related to neurodegenerative diseases.

CK1δ-IN-8 (Compound 429) is a CK1δ inhibitor suitable for Alzheimer's disease research.

Casein kinase1δ-IN-30 (Compound 581) is an inhibitor of casein kinase 1δ (CK1δ). It can be utilized in research related to neurodegenerative diseases.

p38αMAPK/CK1δ inhibitor-1 (Compound 3) exhibits inhibitory activity against p38αMAPK and CK1δ, with IC50 values of 0.185 µM and 0.089 µM, respectively.

Casein kinase1δ-IN-18 (compound 660) is an inhibitor of casein kinase 1δ (CK1δ), which can be utilized for research in neurodegenerative diseases.

IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDAC. It exhibits high selectivity for CK2 with an IC50 of 1.7 nM and demonstrates broad inhibitory activity against HDAC (HDAC1, 2, 3, and 6) with IC50 values of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, while showing low activity against HDAC8. IOR-160 modulates critical cell signaling pathways by inhibiting AKT phosphorylation and increasing α-tubulin acetylation. The compound reduces tumor growth and burden through its dual inhibition of CK2/HDAC and is relevant for research on triple-negative breast cancer.

Casein kinase1δ-IN-26 (compound 505) is a potent inhibitor of casein kinase 1δ. This compound is applicable in research related to neurodegenerative disorders such as Alzheimer’s disease.

CK2-IN-10 (31) is an allosteric inhibitor of CK2, applicable in cancer research.

KDX1381 is a bivalent CK2α inhibitor with an IC50 of 17 nM and a KD of 54 nM. It demonstrates antitumor activity in murine 786-O and A375 xenograft models. Furthermore, when combined with a vascular endothelial growth factor receptor (VEGFR) inhibitor or DNA-damaging agents, KDX1381 enhances antitumor effects in mouse hepatocellular carcinoma and glioma models.

DEG-35 is a CRBN-dependent bifunctional degrader targeting IKZF2 and CK1α, with DC50 values of 1.4 nM and 4.4 nM for CK1α and IKZF2, respectively. It activates the p53 apoptotic pathway and is applicable for research related to acute myeloid leukemia (AML).

AMG-548 dihydrochloride, an oral p38α inhibitor (Ki: 0.5 nM), selectively targets p38β, γ, δ, inhibits TNFα (IC50: 3 nM), and suppresses Wnt signaling.

TMX-4116 is a CK1α degrader targeting multiple cell lines with DC50s below 200 nM, used in multiple myeloma research and protein degradation strategy studies.

Casein kinase1δ-IN-19 (compound 492) is a potent inhibitor of casein kinase 1δ. It is utilized in research related to neurodegenerative disorders, such as Alzheimer's disease.

AMG-548 hydrochloride: orally active, p38α inhibitor (Ki=0.5 nM), 1000x less for p38γ/δ, also blocks TNFα (IC50=3 nM) & inhibits casein kinase 1 δ/ε.

Casein kinase1δ-IN-25 (compound 487) is a potent inhibitor of casein kinase1δ. It is applicable in research on neurodegenerative diseases such as Alzheimer's disease.

CK1δ-IN-3 (compound 376) is a CK1δ (casein kinase 1δ) inhibitor that can be used to study neurodegenerative diseases such as Alzheimer's disease.

Dinoxyline is a potent dopamine receptor agonist, with dissociation constants (Ki values) for D1, D2, D3, and D4 receptors being 7 nM, 6 nM, 5 nM, and 43 nM, respectively. It is utilized in neuroscience research.

CK2 inhibitor 3: potent CK2 blocker, IC50 of 280 nM, suppresses tumor cell growth, highly selective among 320 kinases.

CK2 Inhibitor 2, characterized as a potent, selective, and orally active inhibitor of CK2, demonstrates an impressive IC50 value of 0.66 nM.