Casein Kinase

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.

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

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.

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

(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.

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.

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.

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).

BAY-888 is capable of acting on CSNK1A1 (IC50: 1.5 nM) and CSNK1D (IC50: 5.5 nM).

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.

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-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.

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