Caseina chinasi

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.

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.

<p>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.</p>

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.

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.

INNO-220 is an orally active, CRBN-dependent molecular glue degrader that targets CK1α. By degrading CK1α, INNO-220 induces cell cycle arrest at the G0/G1 phase and triggers apoptosis (Apoptosis). It disrupts the assembly and function of the CARD11/BCL10/MALT1 complex, inhibiting the NF-κB signaling pathway in T cells and lymphoma cells with activating mutations in CARD11. INNO-220 offers a novel direction for lymphoma research.

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

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.

<p>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.</p>

<p>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.</p>

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.

<p>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.</p>

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.

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

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.

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